Fe3O4 nanoparticles mediated synthesis of novel spirooxindole ‐dihydropyrimidinone molecules as Hsp90 inhibitors
Novel spirooxindole ‐dihydropyrimidinones were synthesized by Fe3O4 nanoparticles intervened synthesis and their Hsp90 ATPase inhibitory activities were investigated. All compounds showed a moderate to potent ATPase inhibitory profile, with IC50 values ranging from 0.18 to 6.80 µM, Compounds4j,4h,4f, and4i were more active than the standard, geldanamycin. AbstractHeat shock protein 90 (Hsp90) is a validated molecular chaperone considered as the new key recipient for cancer intervention. The current study illustrates the synthesis of novel spirooxindole ‐dihydropyrimidinones (4a –j) by Fe3O4 nanoparticles interven...
Source: Archiv der Pharmazie - November 28, 2018 Category: Drugs & Pharmacology Authors: Srinubabu Maddela,
Ajitha Makula,
Mario D. Galigniana,
Della G. T. Parambi,
Fernando Federicci,
Gisela Mazaira,
Omnia M. Hendawy,
Sanal Dev,
Githa E. Mathew,
Bijo Mathew Tags: FULL PAPER Source Type: research
Design, synthesis, and molecular docking study of benzothiazolotriazine derivatives for anticonvulsant potential
A series of benzothiazolotriazine derivatives (4a –k) was designed, synthesized, and evaluated for their anticonvulsant activity by MES and scPTZ assays. 8 ‐Chloro‐4‐(2‐chlorocyclohexa‐1,5‐dien‐1‐yl)‐2‐((4‐methoxybenzyl)thio)‐10aH‐benzo[4,5]thiazolo[3,2a][1,3,5]triazine4e as the most promising agent in the series indicated that the presence of a methoxy group at the lipophilic aryl ring confers high anticonvulsant potency. AbstractA series of newer benzothiazolotriazine derivatives (4a –k) was designed, synthesized, and characterized as anticonvulsant agents against the two classically used ME...
Source: Archiv der Pharmazie - November 27, 2018 Category: Drugs & Pharmacology Authors: Jannat Ul Firdaus,
Anwar Habib,
Nadeem Siddiqui,
Ozair Alam,
Mohd. Javed Naim,
Sangh Partap,
Meeta Sahu Tags: FULL PAPER Source Type: research
Antidiabetic potential: In vitro inhibition effects of bromophenol and diarylmethanones derivatives on metabolic enzymes
In this study, we studied the inhibitory effects of bromophenol derivatives on aldose reductase (AR), α‐glucosidase, and α‐amylase enzymes. In the bromophenols series, compound1f showed the maximum inhibition effect against AR with aKi value of 0.05 ± 0.01 μM, while compound1d showed the lowest inhibition effect against AR with aKi value of 1.13 ± 0.99 μM. In addition, α‐amylase from porcine pancreas and α‐glucosidase fromSaccharomyces cerevisiae were used as enzymes. In this study, all compounds were tested for the inhibition of the α‐glucosidase enzyme and demonstrated efficient inhibitio...
Source: Archiv der Pharmazie - November 27, 2018 Category: Drugs & Pharmacology Authors: Yeliz Demir,
Parham Taslimi,
Muhammet Serhat Ozaslan,
Necla Oztaskin,
Yasin Çetinkaya,
İlhami Gulçin,
Şükrü Beydemir,
Suleyman Goksu Tags: FULL PAPER Source Type: research
Synthesis, molecular modeling studies, and anticonvulsant evaluation of novel 1 ‐((2‐hydroxyethyl)(aryl)amino)‐N‐substituted cycloalkanecarboxamides and their acetate esters
The 1,1 ‐disubstituted cycloalkane congeners, 1‐((2‐hydroxyethyl)(aryl)amino)‐N‐substituted cycloalkanecarboxamidesIXa –l and their acetate estersXa –l, were synthesized andin vivo tested for anticonvulsant activity. The most potent compounds in the scPTZ screen exhibited higher anticonvulsant potential than the gold standards, phenobarbital and ethosuximide. AbstractA series of 1 ‐((2‐hydroxyethyl)(aryl)amino)‐N‐substituted cycloalkanecarboxamidesIXa –l and their acetate estersXa –l were designed and synthesized as new anticovulsant agents. The evaluation of the anticonvulsant effect was performe...
Source: Archiv der Pharmazie - November 21, 2018 Category: Drugs & Pharmacology Authors: Mohamed N. Aboul ‐Enein,
Aida A. El‐Azzouny,
Kamilia M. Amin,
Mona E. Aboutabl,
Mai I. Abo‐Elmagd Tags: FULL PAPER Source Type: research
Heterocyclic electrophiles as new MurA inhibitors
An 84 ‐membered covalent fragment library containing five‐ and six‐membered heterocycles with six different warheads was developed and characterized in a GSH‐reactivity assay and an aqueous stability test. Mapping their reactivity revealed their potential as covalent warheads. AbstractAn electrophilic fragment library of small heterocycles was developed and characterized in the surrogate GSH ‐reactivity assay and aqueous stability test that revealed their potential as covalent warheads. Screening the library against MurA fromStaphylococcus aureus (MurASA) andEscherichia coli (MurAEC) identified heterocyclic fragm...
Source: Archiv der Pharmazie - November 21, 2018 Category: Drugs & Pharmacology Authors: Aaron Keeley,
P éter Ábrányi‐Balogh,
Martina Hrast,
Tímea Imre,
Janez Ilaš,
Stanislav Gobec,
György M. Keserű Tags: FULL PAPER Source Type: research
Synthesis and antimycobacterial activity of (+) ‐usnic acid conjugates
Seventeen conjugates of (+) ‐usnic acid with selected polar amino acids or amines or with aromatic and heterocyclic hydrazines and hydrazides are described and tested against sensitive and multidrug‐resistant (MDR) mycobacteria strains. DerivativesPS14 andPS18 showed potent activity against MDRMycobacterium tuberculosis strains, with MIC values comparable to those of other antitubercular drugs already in use for tuberculosis treatment. AbstractNew therapeutics are urgently needed to fight tuberculosis and mycobacteria ‐related diseases that are a major health hazard especially in poor countries. Natural products have...
Source: Archiv der Pharmazie - November 8, 2018 Category: Drugs & Pharmacology Authors: Daniela Cirillo,
Emanuele Borroni,
Irene Festoso,
Diego Monti,
Sergio Romeo,
Dominique Mazier,
Luisella Verotta Tags: FULL PAPER Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (11/2018)
Archiv der Pharmazie,Volume 351, Issue 11, November 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - November 5, 2018 Category: Drugs & Pharmacology Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (11/2018)
Archiv der Pharmazie,Volume 351, Issue 11, November 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - November 5, 2018 Category: Drugs & Pharmacology Source Type: research
Synthesis of some novel quinazolin ‐4(3H)‐one hybrid molecules as potent urease inhibitors
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 30, 2018 Category: Drugs & Pharmacology Authors: Emre Mente şe,
Gülay Akyüz,
Fatih Yılmaz,
Nimet Baltaş,
Mustafa Emirik Source Type: research
Cytotoxicity of new pyridazin ‐3(2H)‐one derivatives orchestrating oxidative stress in human triple‐negative breast cancer (MDA‐MB‐468)
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 29, 2018 Category: Drugs & Pharmacology Authors: Najat Bouchmaa,
Reda Ben Mrid,
Youness Boukharsa,
Mohamed Nhiri,
Hassan Ait Mouse,
Jamal Taoufik,
M'hammed Ansar,
Abdelmajid Zyad Source Type: research
Synthesis and anticancer activity of novel rapamycin C ‐28 containing triazole moiety compounds
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 25, 2018 Category: Drugs & Pharmacology Authors: Qingwen Huang,
Lijun Xie,
Xiaoming Chen,
Hui Yu,
Yubing Lv,
XueHui Huang,
Jiayin Ying,
Congshen Zheng,
Yuanrong Cheng,
Jie Huang Source Type: research
Synthesis of androgen receptor antagonists containing a pentafluorosulfanyl (SF5) moiety
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 15, 2018 Category: Drugs & Pharmacology Authors: Jiyu Jin,
Yan Zhou,
Dehua Yang,
Qiumeng Zhang,
Ming ‐Wei Wang,
Wei Lu Source Type: research
Pyrazinoates as antiparasitic agents against Trypanosoma cruzi
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 9, 2018 Category: Drugs & Pharmacology Authors: Camilla I. Vasconcelos,
Marina T. Varela,
Ana C. Torrecilhas,
Jo ão P. S. Fernandes Source Type: research
Donepezil –melatonin hybrids as butyrylcholinesterase inhibitors: Improving binding affinity through varying mode of linking fragments
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 5, 2018 Category: Drugs & Pharmacology Authors: Iwona Łozińska,
Aleksandra Świerczyńska,
Zuzanna Molęda,
Alwin M. Hartman,
Anna K. H. Hirsch,
Zbigniew Czarnocki Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (10/2018)
Archiv der Pharmazie,Volume 351, Issue 10, October 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 4, 2018 Category: Drugs & Pharmacology Source Type: research
