Chemistry Research 
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This page shows you the most recent publications within this specialty of the MedWorm directory. This is page number 21.
Switchable elastin-like polypeptides that respond to chemical inducers of dimerization.
Abstract
Elastin-like polypeptides (ELPs) are protein polymers that reversibly phase separate in response to increased temperature, pressure, concentration, ionic strength, and molecular weight. If it were possible to engineer their phase separation to respond to specific molecular substrates, ELP fusion proteins might be engineered as biosensors, smart biomaterials, diagnostic imaging agents, and targeted therapies. What has been lacking is a strategy to design ELPs to respond to specific substrates. To address this deficiency, we report that ELP fusion proteins phase separate in response to chemical inducers of d...
Source: Biomacromolecules - February 13, 2013 Category: Biochemistry Authors: Dhandhukia JP, Weitzhandler I, Wang W, Mackay JA Tags: Biomacromolecules Source Type: research
Preparation of lipase-coated, stabilized, hydrophobic magnetic particles for reversible conjugation of biomacromolecules.
Abstract
This communication presents the development of a novel strategy for the easy conjugation of biomolecules to hydrophobic magnetic microparticles via reversible coating with previously functionalized lipase molecules. First, the ability of lipase to be strongly adsorbed onto hydrophobic surfaces was exploited for the stabilization of microparticles in aqueous medium by the creation of a hydrophilic surface. Second, the surface amino acids of lipase can be tailored to suit biomolecule conjugation. This approach has been demonstrated by amino-epoxy activation of lipase, enabling the conjugation of different bi...
Source: Biomacromolecules - February 13, 2013 Category: Biochemistry Authors: Marciello M, Bolivar JM, Filice M, Mateo C, Guisán JM Tags: Biomacromolecules Source Type: research
Species Identification of Cannabis sativa Using Real-Time Quantitative PCR (qPCR)(,).
Abstract
Most narcotics-related cases in the United States involve Cannabis sativa. Material is typically identified based on the cystolithic hairs on the leaves and with chemical tests to identify of the presence of cannabinoids. Suspect seeds are germinated into a viable plant so that morphological and chemical tests can be conducted. Seed germination, however, causes undue analytical delays. DNA analyses that involve the chloroplast and nuclear genomes have been developed for identification of C. sativa materials, but they require several nanograms of template DNA. Using the trnL 3' exon-trnF intragenic spacer ...
Source: Journal of Forensic Sciences - February 13, 2013 Category: Forensic Medicine Authors: Johnson CE, Premasuthan A, Satkoski Trask J, Kanthaswamy S Tags: J Forensic Sci Source Type: research
Composition and Distribution of Elements and Ultrastructural Topography of a Human Cardiac Calculus.
Abstract
Trace elements (TEs) may contribute to the formation of calculi or stones or be involved in the aetiopathogenesis of stone diseases. The compositions and spatial distribution of elements from the inner nucleus to outer crust of the cardiac calculus were investigated by energy-dispersive X-ray fluorescence (EDXRF) spectrometer. The surface topograph, distribution map of elements, elemental and chemical compositions were also determined by environmental scanning electron microscope (ESEM)-energy-dispersive X-ray (EDX) analysis. Twenty-five elements were identifiable from 18 positions on the cardiac calculus ...
Source: Biological Trace Element Research - February 13, 2013 Category: Biology Authors: Cheng CL, Chang HH, Huang PJ, Chu YT, Lin SY Tags: Biol Trace Elem Res Source Type: research
SIRT1 regulates the neurogenic potential of neural precursors in the adult subventricular zone and hippocampus
Abstract
Within the two neurogenic niches of the adult mammalian brain, i.e., the subventricular zone lining the lateral ventricle and the subgranular zone of the hippocampus, there exist distinct populations of proliferating neural precursor cells that differentiate to generate new neurons. Numerous studies have suggested that epigenetic regulation by histone‐modifying proteins is important in guiding precursor differentiation during development; however, the role of these proteins in regulating neural precursor activity in the adult neurogenic niches remains poorly understood. Here we examine the role of an NAD+‐depe...
Source: Journal of Neuroscience Research - February 13, 2013 Category: Neuroscience Authors: Sumiti Saharan, Dhanisha J. Jhaveri, Perry F. Bartlett Tags: Research Article Source Type: research
The contribution of N2O3 to the cytotoxicity of the nitric donor drug DETA/NO; an emerging role for S-nitrosylation.
The objectives of this study were to investigate the influence of oxygen tension on the cytotoxicity of the NO˙ donor DETA/NO and to determine the effects of oxygen tension on the key reactive nitrogen species responsible for any subsequent toxicity. The findings presented in this study indicate that the DETA/NO-mediated cytotoxic effects were enhanced under hypoxic conditions. Further investigations revealed that neither peroxynitrite nor nitroxyl was generated. Fluorometric analysis in the presence of scavengers suggest for the first time that another reactive nitrogen species, dinitrogen trioxide may be responsible for...
Source: Bioscience Reports - February 13, 2013 Category: Biomedical Science Authors: Ali AA, Coulter JA, Ogle CH, Migaud MM, Hirst DG, Robson T, McCarthy HO Tags: Biosci Rep Source Type: research
Access to Organometallic Arylcobaltcorrins through Radical Synthesis: 4-Ethylphenylcobalamin, a Potential "Antivitamin B(12) "
Abstract
Locked B(12) : 4-Ethylphenylcobalamin, a novel organometallic arylcobalamin, has been synthesized in a radical reaction. This vitamin B(12) antimetabolite features a strong CoC bond, and represents a "locked" form of vitamin B(12) . It may be used in animal studies to induce functional vitamin B(12) deficiency artificially to help clarify still controversial issues related to the pathophysiology of vitamin B(12) deficiency.
PMID: 23404623 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Ruetz M, Gherasim C, Gruber K, Fedosov S, Banerjee R, Kräutler B Tags: Angew Chem Int Ed Engl Source Type: research
Stabilized Transient R(2) PN Species.
Abstract
Finally isolated: The isolation of a nitridophosphane(V) was described for the first time by the research group of Bertrand. The reactivity and the possibility of stabilizing labile R(2) PN/R(2) NP species are discussed.
PMID: 23404754 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Schulz A, Villinger A Tags: Angew Chem Int Ed Engl Source Type: research
Mild and Rapid Pd-Catalyzed Cross-Coupling with Hydrazine in Continuous Flow: Application to the Synthesis of Functionalized Heterocycles.
Abstract
Minimizing risk: The synthesis of arylhydrazines through CN cross-coupling of aryl chlorides with hydrazine is described. Through the use of continuous flow, the hazards associated with the use of hydrazine in the presence of transition metals are decreased. In addition, multistep flow sequences have also been developed for the generation of functionalized heterocycles utilizing the arylhydrazine intermediates.
PMID: 23404773 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Deangelis A, Wang DH, Buchwald SL Tags: Angew Chem Int Ed Engl Source Type: research
Palladium-Catalyzed Oxidative Cross-Coupling between Heterocycles and Terminal Alkynes with Low Catalyst Loading.
Abstract
Direct: With [Pd(2) (dba)(3) ] as a catalyst, the direct alkynylation of thiophenes bearing a variety of substituents has been accomplished by using terminal alkynes as alkynylating reagents. This protocol is also applicable to other electron-rich aromatic heterocycles. dba=dibenzylidenacetone.
PMID: 23404782 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Jie X, Shang Y, Hu P, Su W Tags: Angew Chem Int Ed Engl Source Type: research
Self-Assembling Enzyme Networks-A New Path towards Multistep Bioelectrocatalytic Systems.
Abstract
Enzymes for energy: Recently, an elegant and efficient protein-engineering approach was proposed to create self-assembling enzyme arrays. This approach paves the way for efficient biofuel cells and for complex bioelectrocatalytic processes (general scheme shown; blue: enzyme, red: substrate, green: product).
PMID: 23404795 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Schröder U Tags: Angew Chem Int Ed Engl Source Type: research
Telechelic Polyethylene from Catalyzed Chain-Growth Polymerization.
Abstract
A functional chain transfer agent, bis(10-undecenyl)magnesium, was employed as cocatalyst in conjunction with [(C(5) Me(5) )(2) NdCl(2) Li(OEt(2) )(2) ] to catalyze polyethylene (PE) chain growth on magnesium. Vinyl-PE-Mg-PE-vinyl units were then further functionalized. This is the first example of catalytic ethylene polymerization with single-step, in situ functionalization to telechelic polyethylenes.
PMID: 23404812 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: German I, Kelhifi W, Norsic S, Boisson C, D'Agosto F Tags: Angew Chem Int Ed Engl Source Type: research
Enantioselective Separation on Naturally Chiral Metal Surfaces: d,l-Aspartic Acid on Cu(3,1,17)(R&S) Surfaces.
Enantioselective Separation on Naturally Chiral Metal Surfaces: d,l-Aspartic Acid on Cu(3,1,17)(R&S) Surfaces.
Angew Chem Int Ed Engl. 2013 Feb 13;
Authors: Yun Y, Gellman AJ
Abstract
Unequivocal evidence of enantioselective, equilibrium separation of a racemic mixture on a naturally chiral metal surface is presented for the first time. The enantioselectivity is much higher than that of chiral molecules on mineral surfaces. Furthermore, the quantitative nature of the (13) C labeling method provides the first direct measure of an enantiospecific adsorption energy difference on a chiral metal surface.
...
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Yun Y, Gellman AJ Tags: Angew Chem Int Ed Engl Source Type: research
Promoting the Activity of Catalysts for the Oxidation of Water with Bridged Dinuclear Ruthenium Complexes.
Abstract
Solar fuels: Dinuclear ruthenium catalysts prepared from two covalently bridged monomeric catalytic units show outstanding activities towards the oxidation of water with high turnover numbers up to 43 000 and turnover frequencies up to 40 s(-1) . Direct comparison of the performance parameters indicates that the dimers are significantly more active as catalysts than the monomers.
PMID: 23404836 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Jiang Y, Li F, Zhang B, Li X, Wang X, Huang F, Sun L Tags: Angew Chem Int Ed Engl Source Type: research
Asymmetric Synthesis of β-Amino Nitriles through a Sc(III) -Catalyzed Three-Component Mannich Reaction of Silyl Ketene Imines.
Abstract
A range of β-amino nitriles containing contiguous tertiary and quaternary stereogenic carbon centers were synthesized by using the title reaction. The reaction was catalyzed by a chiral N,N'-dioxide scandium(III) complex under mild reaction conditions. Based on experimental investigations, a possible transition state has been proposed to explain the origin of asymmetric inductivity.
PMID: 23404866 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Zhao J, Liu X, Luo W, Xie M, Lin L, Feng X Tags: Angew Chem Int Ed Engl Source Type: research
Perhalogenated Carba-closo-dodecaborate Anions as Ligand Substituents: Applications in Gold Catalysis.
Abstract
Bigger and better! The single-component zwitterionic gold catalyst formed by the coordination of a phosphine ligand bearing an inert and noncoordinating carborane substituent, CB(11) Cl(11) (-) , to an Au(I) ion exhibited the highest reported activity for the hydroamination of alkynes with amines. The highest turnover number observed for hydroamination with this catalyst exceeded a stunning 95 000.
PMID: 23404892 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Lavallo V, Wright JH, Tham FS, Quinlivan S Tags: Angew Chem Int Ed Engl Source Type: research
Cs(2) B(4) SiO(9) : A Deep-Ultraviolet Nonlinear Optical Crystal.
Abstract
Nonlinear optics: A new borosilicate, Cs(2) B(4) SiO(9) , has been synthesized. This compound represents a new kind of a boron-rich borosilicate and shows a 4.6 times stronger powder second-harmonic generation response relative to KH(2) PO(4) . In addition, Cs(2) B(4) SiO(9) has a short UV cutoff edge (below 190 nm).
PMID: 23404912 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Wu H, Yu H, Pan S, Huang Z, Yang Z, Su X, Poeppelmeier KR Tags: Angew Chem Int Ed Engl Source Type: research
Design, Synthesis, and Biological Evaluation of Truncated Superstolide A.
Abstract
By design: A truncated superstolide A, a simplified analogue of the potent anticancer marine macrolide superstolide A, was designed and successfully synthesized by a highly efficient and convergent approach. The biological evaluation showed that this compound maintains the potent anticancer activity of the original natural product superstolide A.
PMID: 23404936 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Chen L, Riaz Ahmed KB, Huang P, Jin Z Tags: Angew Chem Int Ed Engl Source Type: research
Pot Economy in the Synthesis of Prostaglandin A(1) and E(1) Methyl Esters.
Pot Economy in the Synthesis of Prostaglandin A(1) and E(1) Methyl Esters.
Angew Chem Int Ed Engl. 2013 Feb 13;
Authors: Hayashi Y, Umemiya S
Abstract
Pot luck: Prostaglandins regulate a broad range of physiological processes and some of their derivatives are used as effective drugs, but previously their preparation has required many steps. The title compounds were efficiently synthesized in a small number of synthetic steps by using a recently developed organocatalyst and practical, one-pot operations involving several successive reactions.
PMID: 23404945 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Hayashi Y, Umemiya S Tags: Angew Chem Int Ed Engl Source Type: research
Bypassing the Limitations of Classical Chemical Purification with DNA-Programmable Nanoparticle Recrystallization.
Abstract
And then there was one: Anisotropic nanoparticle syntheses often contain impurity nanostructures. Functionalization of the products of such syntheses with DNA (see scheme (1)) allows the relative interaction strengths between particles to be tailored. The desired nanoparticle component can then be crystallized selectively (2) and separated to arrive at samples of significantly improved purity (3).
PMID: 23404954 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - February 13, 2013 Category: Chemistry Authors: Jones MR, Mirkin CA Tags: Angew Chem Int Ed Engl Source Type: research
Forensic toxicology.
PMID: 23404129 [PubMed - as supplied by publisher]
Source: Analytical and Bioanalytical Chemistry - February 13, 2013 Category: Chemistry Authors: Watanabe K, Chinaka S Tags: Anal Bioanal Chem Source Type: research
Validation and transferability study of a method based on near-infrared hyperspectral imaging for the detection and quantification of ergot bodies in cereals.
Abstract
In recent years, near-infrared (NIR) hyperspectral imaging has proved its suitability for quality and safety control in the cereal sector by allowing spectroscopic images to be collected at single-kernel level, which is of great interest to cereal control laboratories. Contaminants in cereals include, inter alia, impurities such as straw, grains from other crops, and insects, as well as undesirable substances such as ergot (sclerotium of Claviceps purpurea). For the cereal sector, the presence of ergot creates a high toxicity risk for animals and humans because of its alkaloid content. A study was undertak...
Source: Analytical and Bioanalytical Chemistry - February 13, 2013 Category: Chemistry Authors: Vermeulen P, Fernández Pierna JA, van Egmond HP, Zegers J, Dardenne P, Baeten V Tags: Anal Bioanal Chem Source Type: research
Nanoscale surface analysis on second generation advanced high strength steel after hot dip galvanizing.
Abstract
Second generation advanced high strength steel is one promising material of choice for modern automotive structural parts because of its outstanding maximal elongation and tensile strength. Nonetheless there is still a lack of corrosion protection for this material due to the fact that cost efficient hot dip galvanizing cannot be applied. The reason for the insufficient coatability with zinc is found in the segregation of manganese to the surface during annealing and the formation of manganese oxides prior coating. This work analyses the structure and chemical composition of the surface oxides on so called...
Source: Analytical and Bioanalytical Chemistry - February 13, 2013 Category: Chemistry Authors: Arndt M, Duchoslav J, Preis K, Samek L, Stifter D Tags: Anal Bioanal Chem Source Type: research
Combination of preparative HPLC and HSCCC methods to separate phosphodiesterase inhibitors from Eucommia ulmoides bark guided by ultrafiltration-based ligand screening.
Abstract
Phosphodiesterase (PDE) inhibitors are widely used because of their various pharmacological properties, and natural products are considered the most productive source of PDE inhibitors. In this work, a new ultrafiltration-high-performance liquid chromatography (HPLC)-diode-array detection-mass spectrometry based ligand screening was developed for the first screening of PDE inhibitors from Eucommia ulmoides bark, and then the target bioactive compounds were prepared by combination of stepwise preparative HPLC and high-speed countercurrent chromatography (HSCCC) methods. Experiments were conducted to optimiz...
Source: Analytical and Bioanalytical Chemistry - February 13, 2013 Category: Chemistry Authors: Shi SY, Peng MJ, Zhang YP, Peng S Tags: Anal Bioanal Chem Source Type: research
Anion-induced changes of structure interpenetration and magnetic properties in 3D Dy-Cu metal-organic frameworks.
Abstract
Two novel Dy-Cu MOFs were structurally and magnetically characterized. The results reveal that it is the first example of anion-induced change of structure interpenetration and magnetic properties in 3d-4f MOFs.
PMID: 23403449 [PubMed - as supplied by publisher]
Source: Chemical Communications - February 13, 2013 Category: Chemistry Authors: Shi PF, Xiong G, Zhao B, Zhang ZY, Cheng P Tags: Chem Commun (Camb) Source Type: research
A yolk-shell structured Fe(2)O(3)@mesoporous SiO(2) nanoreactor for enhanced activity as a Fenton catalyst in total oxidation of dyes.
Abstract
Through a simple polymeric carbon assisted method, a yolk-shell structured Fe(2)O(3)@mesoporous SiO(2) nanoreactor was synthesized and showed excellent activity in Fenton-like reactions toward methylene blue total degradation.
PMID: 23403459 [PubMed - as supplied by publisher]
Source: Chemical Communications - February 13, 2013 Category: Chemistry Authors: Cui ZM, Chen Z, Cao CY, Jiang L, Song WG Tags: Chem Commun (Camb) Source Type: research
Homogeneous electrochemical aptamer-based ATP assay with signal amplification by exonuclease III assisted target recycling.
Abstract
A novel and homogeneous electrochemical aptamer-based adenosine triphosphate (ATP) assay was demonstrated with signal amplification by exonuclease III-assisted target recycling. A superior detection limit of 1 nM toward ATP with an excellent selectivity could be achieved.
PMID: 23403496 [PubMed - as supplied by publisher]
Source: Chemical Communications - February 13, 2013 Category: Chemistry Authors: Liu S, Wang Y, Zhang C, Lin Y, Li F Tags: Chem Commun (Camb) Source Type: research
Gyroidal metal-organic frameworks by solvothermal subcomponent self-assembly.
Abstract
Solvothermal subcomponent self-assembly has been employed as a convenient and advanced route to prepare metal-organic frameworks (MOFs). A new gyroidal MOF with gie topology was successfully synthesized and characterized; gas adsorption properties were also investigated.
PMID: 23403513 [PubMed - as supplied by publisher]
Source: Chemical Communications - February 13, 2013 Category: Chemistry Authors: Wu Y, Zhou XP, Yang JR, Li D Tags: Chem Commun (Camb) Source Type: research
Atmospheric microplasma-functionalized 3D microfluidic strips within dense carbon nanotube arrays confine Au nanodots for SERS sensing.
Abstract
An atmospheric microplasma jet produces three-dimensional (3D) microfluidic channels on dense arrays of vertically aligned carbon nanotubes, which confines Au nanodot aqueous solution. The resulting hybrid 3D nanostructure is exploited as an effective microscopic area-selective sensing platform based on surface-enhanced Raman scattering.
PMID: 23404040 [PubMed - as supplied by publisher]
Source: Chemical Communications - February 13, 2013 Category: Chemistry Authors: Yick S, Han ZJ, Ostrikov KK Tags: Chem Commun (Camb) Source Type: research
Characterization of bacteriocin bificin C6165: a novel bacteriocin
ConclusionsBificin C6165 is indeed a novel bacteriocin and it exhibited remarkable potency for Alicyclobacillus control.
Significance and Impact of the StudyApplication of bacteriocins in preservation of fruit juices has seldom been studied. Bificin C6165 may be an alternative method to control juice spoilage by this Alicyclobacillus acidoterrestris and meet increasing consumer demand for nature and artificial chemical additive‐free food products.
Source: Journal of Applied Microbiology - February 13, 2013 Category: Microbiology Authors: J. Pei, Y. Yuan, T. Yue Tags: Original Article Source Type: research
Design, Synthesis and Structure–Activity Relationship of New Arginine Vasopressin Analogues Containing Proline Derivatives in Position 2
In this study, we present the synthesis and pharmacological properties of new analogues of arginine vasopressin modified in the N‐terminal part of the molecule with proline derivatives: indoline‐2‐carboxylic acid (Ica) and (2S,4R)‐4‐(naphthalene‐2‐ylmethyl)pyrrolidine‐2‐carboxylic acid. All the peptides were tested for pressor, antidiuretic and in vitro uterotonic activities. We also determined their binding affinity to the human oxytocin receptor. The Ica2 substitution resulted in two moderately potent and selective antioxytocic agents: [Mpa1, Ica2, D‐Arg8]VP and [Mpa1,Ica2,Val4,D‐Arg8]VP (pA2 = ...
Source: Chemical Biology and Drug Design - February 13, 2013 Category: Biology Authors: Anna Kwiatkowska, Monika Lewandowska, Lenka Borovičková, Jiřina Slaninová, Bernard Lammek, Adam Prahl Tags: Research Letter Source Type: research
Design and Evaluation of 4‐Aminophenol and Salicylate Derivatives as Free‐Radical Scavenger
This theoretical and experimental study describes the design and evaluation of the free‐radical scavenging effect for the molecular association of 4‐aminophenol and salicylate derivatives. For this purpose, we employed theoretical methods for the selection of antioxidant drugs and the rapid methods of evaluation: the 1,1‐diphenyl‐2‐picrylhydrazyl radical and the thiobarbituric acid reactive substances in the lipid peroxidation initiated by Fe2+ and ascorbic acid in human erythrocytes. The associate derivatives exhibited a more potent inhibition than the salicylic acid, while the benzoyl compound exhibited a more ...
Source: Chemical Biology and Drug Design - February 13, 2013 Category: Biology Authors: Rosivaldo S. Borges, Glaécia A. N. Pereira, Joyce K. L. Vale, Luiz C. S. França, Marta C. Monteiro, Cláudio N. Alves, Albérico B. F. da Silva Tags: Research Article Source Type: research
Identification of Small Molecule Hes1 Modulators as Potential Anticancer Chemotherapeutics
Hes1 is a key transcriptional regulator primarily controlled by the Notch signaling pathway, and recent studies have demonstrated both an oncogenic and tumor suppressor role for Hes1, depending on the cell type. Small molecules that activate and inhibit Hes1 activity hold promise as future anticancer chemotherapeutics. We have utilized a cell‐based dual luciferase assay to identify modulators of Hes1 expression in a medium‐throughput format. A modest screen was performed in HCT‐116 colon cancer cell lines, and two small molecules were identified and characterized as Hes1 regulators. Compound 3 induced Hes1 expression...
Source: Chemical Biology and Drug Design - February 13, 2013 Category: Biology Authors: Vibhavari Sail, M. Kyle Hadden Tags: Research Article Source Type: research
Issue Information
Source: Chemical Biology and Drug Design - February 13, 2013 Category: Biology Source Type: research
Indolizine derivatives as HIV‐1 VIF‐ElonginC interaction inhibitors
Abstract
Compound 1 (VEC‐5) was identified as a potent small molecular HIV‐1 VIF inhibitor that targets the VIF‐ElonginC interaction. A structure‐activity relationship study was carried out to develop compounds with improved efficacy against HIV‐1 and 49 indolizine derivatives of three categories were designed and synthesized. We found that 5 compounds exhibited promising anti‐HIV‐1 activity and the most active compound 2g had an IC50 value of 11.0 μM. These results provide new information to develop highly potent small‐molecule HIV‐1 VIF inhibitors.
© 2013 John Wiley & Sons A/S
Source: Chemical Biology and Drug Design - February 13, 2013 Category: Biology Authors: Wenlin Huang, Tao Zuo, Xiao Luo, Hongwei Jin, Zhenming Liu, Zhenjun Yang, Xianghui Yu, Liangren Zhang, Lihe Zhang Tags: Research Article Source Type: research
Basic surface-active properties in the homologous series of beta-alkyl (C12H25/C18H37) polyethyleneoxy (n = 0-20) propionamides
Conclusions:
The idea of the obtaining and basic colloidal characterization of heterogeneous R(EO)nPD is justified. The knowledge and constructive approach of the heterogeneous character confirm the basic surface-active potential of R(EO)nPD, the structure-colloidal characteristics dependence and justifies further, more extensive research.
Source: Chemistry Central Journal - February 13, 2013 Category: Chemistry Authors: Adrian Rivi¿Gabriel BujancaTeodor Tra¿c¿ Source Type: research
The human is an exception to the evolutionarily-conserved phenomenon of pre-fertilization zona pellucida resistance to proteolysis induced by oviductal fluid
STUDY QUESTION
Is zona pellucida (ZP) resistance to proteolysis, induced by oviductal fluid (OF), a mechanism common to species other than the pig and cow?
Summary Answer
ZP resistance to proteolysis induced by OF was observed in the mouse, rat, hamster, rabbit, sheep, goat, pig and cow, but not in humans.
WHAT IS KNOWN ALREADY
Oviductal ZP resistance to proteolysis occurs in the pig and cow where it influences the incidence of fertilization and polyspermy. The effect is observed after incubation of ZP in OFs from pig (pOF), cow (cOF), rabbit (rOF) and sheep (sOF).
STUDY DESIGN, SIZE, DURATION
Oocytes from nine differen...
Source: Human Reproduction - February 13, 2013 Category: Reproduction Medicine Authors: Mondejar, I., Aviles, M., Coy, P. Tags: Reproductive biology Source Type: research
Environmental oestrogens and breast cancer: long-term low-dose effects of mixtures of various chemical combinations
The incidence of breast cancer has risen worldwide to unprecedented levels in recent decades, making it now the major cancer of women in many parts of the world.1 Although diet, alcohol, radiation and inherited loss of BRCA1/2 genes have all been associated with increased incidence, the main identified risk factors are life exposure to hormones including physiological variations associated with puberty/pregnancy/menopause,1 personal choice of use of hormonal contraceptives2 and/or hormone replacement therapy.3–6 On this basis, exposure of the human breast to the many environmental pollutant chemicals capable of mimic...
Source: Journal of Epidemiology and Community Health - February 13, 2013 Category: Epidemiology Authors: Darbre, P. D., Fernandez, M. F. Tags: Epidemiologic studies, Case-control studies, Environmental issues Editorials Source Type: research
Behavioural and genetic analyses of Nasonia shed light on the evolution of sex pheromones
Nature advance online publication 13 February 2013. doi:10.1038/nature11838
Authors: Oliver Niehuis, Jan Buellesbach, Joshua D. Gibson, Daniela Pothmann, Christian Hanner, Navdeep S. Mutti, Andrea K. Judson, Jürgen Gadau, Joachim Ruther & Thomas Schmitt
Sex pheromones play a pivotal role in the communication of many sexually reproducing organisms. Accordingly, speciation is often accompanied by pheromone diversification enabling proper mate finding and recognition. Current theory implies that chemical signals are under stabilizing selection by the receivers who thereby maintain the integrity of the signals. How t...
Source: Nature AOP - February 13, 2013 Category: Research Authors: Oliver NiehuisJan BuellesbachJoshua D. GibsonDaniela PothmannChristian HannerNavdeep S. MuttiAndrea K. JudsonJürgen GadauJoachim RutherThomas Schmitt Tags: Letter Source Type: research
Simple organic molecules as catalysts for enantioselective synthesis of amines and alcohols
Amir H. Hoveyda
The discovery of catalysts that can be used to synthesize complex organic compounds by enantioselective transformations is central to advances in the life sciences; for this reason, many chemists aim to discover catalysts that allow for preparation of chiral molecules as predominantly one mirror-image isomer. The ideal catalyst should not contain precious elements and should bring reactions to completion in a few hours through operationally simple procedures. Here we introduce a set of small organic molecules that can catalyse reactions of unsaturated organoboron reagents with imines and carbonyls; th...
Source: Nature - February 13, 2013 Category: Research Authors: Daniel L. SilverioSebastian TorkerTatiana PilyuginaErika M. VieiraMarc L. SnapperFredrik HaeffnerAmir H. Hoveyda Tags: Letter Source Type: research
MMP‐3 mediates psychosine‐induced globoid cell formation: Implications for leukodystrophy pathology
Abstract
Globoid cell leukodystrophy (GLD) or Krabbe disease, is a fatal demyelinating disease attributed to mutations in the galactocerebrosidase (GALC) gene. Loss of function mutations in GALC result in accumulation of the glycolipid intermediate, galactosylsphingosine (psychosine). Due to the cytotoxicity of psychosine, it has been hypothesized that accumulated psychosine underlie the pathophysiology of GLD. However, the cellular mechanisms of GLD pathophysiology remain unclear. Globoid cells, multinucleated microglia/macrophages in the central nervous system (CNS), are a defining characteristic of GLD. Here we report t...
Source: Glia - February 13, 2013 Category: Neurology Authors: Kumiko Ijichi, Graham D. Brown, Craig S. Moore, Jean‐Pyo Lee, Paige N. Winokur, Roberto Pagarigan, Evan Y. Snyder, Ernesto R. Bongarzone, Stephen J. Crocker Tags: Original Article Source Type: research
Suppression of Chloride Channel 3 Expression Facilitates Sensitivity of Human Glioma U251 Cells to Cisplatin Through Concomitant Inhibition of Akt and Autophagy
In this study, we investigated the role of chloride channel‐3 (ClC‐3) in cisplatin resistance. Autophagy was demonstrated by accumulation of LC3‐II, beclin 1 and Atg12‐Atg5. The ultrastructure changes were observed under electron microscope. Chemical staining with acridine orange or MDC was used to detect acidic vesicular organelles. Quantification of apoptosis was detected by PI and Annexin V staining. The mechanisms involved in the Akt pathway and autophagy were studied by western blot analysis. Our results showed that Akt phosphorylation and autophagy were induced by cisplatin in human glioma U251 cells. Specifi...
Source: The Anatomical Record Part B: The New Anatomist - February 13, 2013 Category: Anatomy Authors: Jing Su, Ye Xu, Lei Zhou, Hui‐Mei Yu, Jin‐Song Kang, Ning Liu, Cheng‐Shi Quan, Lian‐Kun Sun Tags: Full Length Article Source Type: research
Discovery of novel biomarkers and phenotypes by semantic technologies
Conclusions:
The reported approach of employing autonomous self-organising semantic engines to aid biomarker discovery, supplemented by appropriate manual curation processes, shows promise and has potential to impact, conservatively, a faster alternative to vocabulary processes dependent on humans having to read and analyze all the texts. More optimistically, it could impact pharmaceutical research, for example to shorten time-to-market of novel drugs, or speed up early recognition of dead ends and adverse reactions.
Source: BMC Bioinformatics - Latest articles - February 13, 2013 Category: Bioinformatics Authors: Carlo TrugenbergerChristoph WältiDavid PeregrimMark SharpSvetlana Bureeva Source Type: research
Fluconazole–malonic acid (1/1)
Co-crystallizaton of the antifungal drug fluconazole [2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol] with malonic acid in acetonitrile solution resulted in the formation of the title 1:1 co-crystal, C13H12F2N6O·C3H4O4. The geometry around the central fluconazole atom is distorted tetrahedral. The dihedral angles between the triazole rings and the fluorinated phenyl ring are 30.64 (7) and 61.91 (5)°. In the crystal, the basic packing motif may be envisioned as a cyclic aggregate formed of two fluconazole molecules linked by two malonic acid molecules through O—H...N and O—H...O hydrogen bonds. S...
Source: Acta Crystallographica Section E - February 13, 2013 Category: Chemistry Authors: Kastelic, J.Kikelj, D.Leban, I.Lah, N. Tags: organic compounds Source Type: research
2-(2,4-Dichlorophenoxymethyl)-5-(4-methylphenyl)imidazo[2,1-b][1,3,4]thiadiazoleAdditional correspondence author, e-mail: bakrfatehy@yahoo.com.
In the title compound, C18H13Cl2N3OS, the eight atoms comprising the central imidazo/thiadiazolethiadiazole residue are coplanar (r.m.s. deviation = 0.009 Å). The dihedral angle of 8.72 (13)° between the dichlorobenzene and tolyl rings reflects a twist about the O—C(benzene) bond; the Cm—O—Cb—Cb torsion angle = −168.5 (2)° (m = methylene C and b is benzene C). Supramolecular tapes along the b axis are found in the crystal structure which are mediated by π–π interactions occurring between centrosymmetrically related thiadiazole rings [inter-ring centroid distance = 3.6907 (16) Å] and between the ...
Source: Acta Crystallographica Section E - February 13, 2013 Category: Chemistry Authors: Abdel-Wahab, B.F.Mohamed, H.A.Ng, S.W.Tiekink, E.R.T. Tags: organic compounds Source Type: research
6,7-Difluoro-1,2,3,4-tetrahydroquinoxaline-5,8-dicarbonitrile
In the title compound, C10H6F2N4, the Car—N bonds are slightly shortened with respect to a standard aniline C—N bond [1.3580 (16) and 1.3618 (16) versus 1.39 Å], thus indicating some π–π conjgation with the electron-acceptor CN groups. The molecule, except for two C atom of the ethylene bridge, is nearly planar, the largest deviation of the other non-H atoms from the mean plane being 0.309 (2) Å. The N—C—C—N torsion angle involving the ethylene bridge is 50.23 (18)°. In the crystal, molecules are connected by pairs of N—H...N hydrogen bonds into chains along [21-1].
Source: Acta Crystallographica Section E - February 13, 2013 Category: Chemistry Authors: Qu, B.-H.Jia, X.-C.Li, J.He, M.-Y. Tags: organic compounds Source Type: research
3,3′-(1-Oxopropane-1,3-diyl)bis(1,3-thiazolidine-2-thione) chlorobenzene hemisolvate
The title compound, C9H12N2OS4·0.5C6H5Cl, which contains two 1,3-thiazolidine-2-thione rings, is a by-product of the synthesis of 3-acryloyl-1,3-thiazolidine-2-thione. The dihedral angle between these rings is 79.95 (9)°, with both rings displaying a twisted conformation. The twist angle of the amide group is 5.6 (1)°. In the crystal, the molecules are linked into [001] chains by C—H...O interactions. The chlorobenzene solvent molecule was found to show unresolvable disorder about a centre of inversion and its contribution to the scattering was removed with the SQUEEZE option in PLATON [Spek (2009). Acta Cryst. D65, 148–155].
Source: Acta Crystallographica Section E - February 13, 2013 Category: Chemistry Authors: Franzel, C.Purdy, A.Butcher, R.J. Tags: organic compounds Source Type: research
Poly[tris(dimethylformamide)(μ3-2,4,6-triiodobenzene-1,3,5-tricarboxylato)samarium(III)]
In the title compound, [Sm(C9I3O6)(C3H7NO)3]n, the SmIII atom is coordinated by nine O atoms, viz. six carboxylate O atoms from three 2,4,6-triiodobenzene-1,3,5-tricarboxylate (I3BTC) ligands and three O atoms from three N,N-dimethylformamide (DMF) molecules. Each I3BTC ligand bridges three SmIII atoms, generating a three-dimensional metal-organic framework structure. The asymmetric unit contains one SmIII ion and one I3BTC anion, both situated on a threefold axis, and one DMF molecule in a general position.
Source: Acta Crystallographica Section E - February 13, 2013 Category: Chemistry Authors: Yan, B.Sheng, D.Yang, Y. Tags: metal-organic compounds Source Type: research
1,3-Dimethyl-1H-1,2,3-benzotriazol-3-ium tetrachloridoferrate(III)
The asymmetric unit of the title salt, (C8H10N3)[FeCl4], contains one 1,3-dimethyl-1H-1,2,3-benzotriazol-3-ium cation and one tetrachloridoferrate anion. The FeIII atom in the anion is tetrahedrally coordinated by four Cl atoms. In the crystal, interactions are observed between the Cl atoms and the triazolium ring [Cl...centroid distances = 3.587 (3) and 3.866 (3) Å].
Source: Acta Crystallographica Section E - February 13, 2013 Category: Chemistry Authors: Sun, Z.Hu, D.-C.Liu, J.-C. Tags: metal-organic compounds Source Type: research
catena-Poly[[(tetrahydrofuran-κO)potassium]-di-μ-dimethylamido-κ4N:N-aluminium-di-μ-dimethylamido-κ4N:N-potassium-di-μ-dimethylamido-κ4N:N-aluminium-di-μ-dimethylamido-κ4N:N]
The title compound, [Al2K2(C2H6N)8(C4H8O)]n, formed during the sonochemical reaction between Al(NMe2)3 and sodium–potassium alloy in the presence of tetrahydrofuran (THF). Its asymmetric unit has two inequivalent K+ sites. One site is coordinated by a THF ligand, and crystallizes as a one-dimensional polymer with a backbone of catenated AlN2K rings. A twofold rotation axis bisects one K+ site and the THF ligand; the second K+ site is situated on an inversion centre, resulting in a planar four-coordination by N atoms. The latter symmetry operation generates the second half of the THF molecule and fills out the coordinatio...
Source: Acta Crystallographica Section E - February 13, 2013 Category: Chemistry Authors: Purdy, A.Parrish, D. Tags: metal-organic compounds Source Type: research
