Synthetic Protocols, Structural Activity Relationship, and Biological Activity of Piperazine and its Derivatives
Med Chem. 2024 Apr 29. doi: 10.2174/0115734064304396240415110015. Online ahead of print.ABSTRACTThe versatile basic structure of piperazine allows for the development and production of newer bioactive molecules that can be used to treat a wide range of diseases. Piperazine derivatives are unique and can easily be modified for the desired pharmacological activity. The two opposing nitrogen atoms in a six-membered piperazine ring offer a large polar surface area, relative structural rigidity, and more acceptors and donors of hydrogen bonds. These properties frequently result in greater water solubility, oral bioavailability,...
Source: Medicinal Chemistry - April 30, 2024 Category: Chemistry Authors: Md Faizan Rajnish Kumar Avijit Mazumder None Salahuddin Neelima Kukreti Arvind Kumar Mvnl Chaitanya Source Type: research
Synthetic Protocols, Structural Activity Relationship, and Biological Activity of Piperazine and its Derivatives
Med Chem. 2024 Apr 29. doi: 10.2174/0115734064304396240415110015. Online ahead of print.ABSTRACTThe versatile basic structure of piperazine allows for the development and production of newer bioactive molecules that can be used to treat a wide range of diseases. Piperazine derivatives are unique and can easily be modified for the desired pharmacological activity. The two opposing nitrogen atoms in a six-membered piperazine ring offer a large polar surface area, relative structural rigidity, and more acceptors and donors of hydrogen bonds. These properties frequently result in greater water solubility, oral bioavailability,...
Source: Medicinal Chemistry - April 30, 2024 Category: Chemistry Authors: Md Faizan Rajnish Kumar Avijit Mazumder None Salahuddin Neelima Kukreti Arvind Kumar Mvnl Chaitanya Source Type: research
Synthetic Protocols, Structural Activity Relationship, and Biological Activity of Piperazine and its Derivatives
Med Chem. 2024 Apr 29. doi: 10.2174/0115734064304396240415110015. Online ahead of print.ABSTRACTThe versatile basic structure of piperazine allows for the development and production of newer bioactive molecules that can be used to treat a wide range of diseases. Piperazine derivatives are unique and can easily be modified for the desired pharmacological activity. The two opposing nitrogen atoms in a six-membered piperazine ring offer a large polar surface area, relative structural rigidity, and more acceptors and donors of hydrogen bonds. These properties frequently result in greater water solubility, oral bioavailability,...
Source: Medicinal Chemistry - April 30, 2024 Category: Chemistry Authors: Md Faizan Rajnish Kumar Avijit Mazumder None Salahuddin Neelima Kukreti Arvind Kumar Mvnl Chaitanya Source Type: research
Synthesis, Molecular Docking Studies and Biological Evaluation of Thiazolyl Hydrazone Derivatives of Chromone-3-carbaldehyde as Potent Anti-Oxidant and Anti-Inflammatory Agents
CONCLUSION: Thus, these compounds represent an attractive template for the evaluation of new antiinflammatory and antioxidant agents and might be useful for exploring new therapeutic tools.PMID:38676527 | DOI:10.2174/0115734064293848240408085039 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 27, 2024 Category: Chemistry Authors: Rakhi Gawali Raghunath Bhosale Rohit Bavi Shravan Jadhav Nargisbano Peerzade Source Type: research
Substituted 4H-3,1-benzoxazine-4-one Derivatives as Inhibitors of Cathepsin G
CONCLUSION: Thus, we propose this inhibitor as a lead molecule to guide subsequent efforts to develop clinically relevant potent and selective CatG inhibitors for use as anti-inflammatory agents.PMID:38676528 | DOI:10.2174/0115734064300678240408084822 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 27, 2024 Category: Chemistry Authors: Kholoud F Aliter Rami A Al-Horani Source Type: research
Synthesis, Molecular Docking Studies and Biological Evaluation of Thiazolyl Hydrazone Derivatives of Chromone-3-carbaldehyde as Potent Anti-Oxidant and Anti-Inflammatory Agents
CONCLUSION: Thus, these compounds represent an attractive template for the evaluation of new antiinflammatory and antioxidant agents and might be useful for exploring new therapeutic tools.PMID:38676527 | DOI:10.2174/0115734064293848240408085039 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 27, 2024 Category: Chemistry Authors: Rakhi Gawali Raghunath Bhosale Rohit Bavi Shravan Jadhav Nargisbano Peerzade Source Type: research
Substituted 4H-3,1-benzoxazine-4-one Derivatives as Inhibitors of Cathepsin G
CONCLUSION: Thus, we propose this inhibitor as a lead molecule to guide subsequent efforts to develop clinically relevant potent and selective CatG inhibitors for use as anti-inflammatory agents.PMID:38676528 | DOI:10.2174/0115734064300678240408084822 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 27, 2024 Category: Chemistry Authors: Kholoud F Aliter Rami A Al-Horani Source Type: research
Synthesis, Molecular Docking Studies and Biological Evaluation of Thiazolyl Hydrazone Derivatives of Chromone-3-carbaldehyde as Potent Anti-Oxidant and Anti-Inflammatory Agents
CONCLUSION: Thus, these compounds represent an attractive template for the evaluation of new antiinflammatory and antioxidant agents and might be useful for exploring new therapeutic tools.PMID:38676527 | DOI:10.2174/0115734064293848240408085039 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 27, 2024 Category: Chemistry Authors: Rakhi Gawali Raghunath Bhosale Rohit Bavi Shravan Jadhav Nargisbano Peerzade Source Type: research
Substituted 4H-3,1-benzoxazine-4-one Derivatives as Inhibitors of Cathepsin G
CONCLUSION: Thus, we propose this inhibitor as a lead molecule to guide subsequent efforts to develop clinically relevant potent and selective CatG inhibitors for use as anti-inflammatory agents.PMID:38676528 | DOI:10.2174/0115734064300678240408084822 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 27, 2024 Category: Chemistry Authors: Kholoud F Aliter Rami A Al-Horani Source Type: research
Unveiling Therapeutic Avenues for Crohn's Disease Management: Exploring Inhibitors for Adherent-Invasive Escherichia coli Propanediol Dehydratase
CONCLUSION: Ultimately, the results of this study have revealed five compounds to possess the potential to serve as inhibitors of pduC of AIEC. However, experimental studies are still needed to validate the findings of this study.PMID:38659270 | DOI:10.2174/0115734064295521240227052730 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 25, 2024 Category: Chemistry Authors: Mohammed Bourhia Md Eram Hosen Md Omar Faruqe Faria Tasnim Mohamed Taibi Amine Elbouzidi Yousef A Bin Jardan Samir Ibenmoussa Abdeslam Asehraou Source Type: research
Unveiling Therapeutic Avenues for Crohn's Disease Management: Exploring Inhibitors for Adherent-Invasive Escherichia coli Propanediol Dehydratase
CONCLUSION: Ultimately, the results of this study have revealed five compounds to possess the potential to serve as inhibitors of pduC of AIEC. However, experimental studies are still needed to validate the findings of this study.PMID:38659270 | DOI:10.2174/0115734064295521240227052730 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 25, 2024 Category: Chemistry Authors: Mohammed Bourhia Md Eram Hosen Md Omar Faruqe Faria Tasnim Mohamed Taibi Amine Elbouzidi Yousef A Bin Jardan Samir Ibenmoussa Abdeslam Asehraou Source Type: research
Unveiling Therapeutic Avenues for Crohn's Disease Management: Exploring Inhibitors for Adherent-Invasive Escherichia coli Propanediol Dehydratase
CONCLUSION: Ultimately, the results of this study have revealed five compounds to possess the potential to serve as inhibitors of pduC of AIEC. However, experimental studies are still needed to validate the findings of this study.PMID:38659270 | DOI:10.2174/0115734064295521240227052730 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - April 25, 2024 Category: Chemistry Authors: Mohammed Bourhia Md Eram Hosen Md Omar Faruqe Faria Tasnim Mohamed Taibi Amine Elbouzidi Yousef A Bin Jardan Samir Ibenmoussa Abdeslam Asehraou Source Type: research
Computational Chemistry: Prediction of Compound Accessibility of Targeted Synthesized Compounds
CONCLUSION: Density functional theory (DFT) investigations emphasize the exceptional stability of complex 3d, which possesses the biggest energy gap and the lowest softness. In contrast, compound 3h demonstrates poorer stability among the tested compounds, characterized by the lowest energy gap and the highest softness values. These findings are further substantiated by absolute energy calculations. The negligible energy difference in compound 3h indicates an increased transfer of electric charge within the molecule, which is associated with its enhanced biological effectiveness. The drug-likeness of the compounds is confi...
Source: Medicinal Chemistry - April 19, 2024 Category: Chemistry Authors: Visagamoorthy Babu Sumeer Ahmed A K Rahiman Sarkar M A Kawsar Malika Berredjem Ajmal R Bhat K Anver Basha Source Type: research
Computational Chemistry: Prediction of Compound Accessibility of Targeted Synthesized Compounds
CONCLUSION: Density functional theory (DFT) investigations emphasize the exceptional stability of complex 3d, which possesses the biggest energy gap and the lowest softness. In contrast, compound 3h demonstrates poorer stability among the tested compounds, characterized by the lowest energy gap and the highest softness values. These findings are further substantiated by absolute energy calculations. The negligible energy difference in compound 3h indicates an increased transfer of electric charge within the molecule, which is associated with its enhanced biological effectiveness. The drug-likeness of the compounds is confi...
Source: Medicinal Chemistry - April 19, 2024 Category: Chemistry Authors: Visagamoorthy Babu Sumeer Ahmed A K Rahiman Sarkar M A Kawsar Malika Berredjem Ajmal R Bhat K Anver Basha Source Type: research
Antimicrobial Potential of Polyphenols: An Update on Alternative for Combating Antimicrobial Resistance
Med Chem. 2024 Apr 5. doi: 10.2174/0115734064277579240328142639. Online ahead of print.ABSTRACTThe last decade has encountered an increasing demand for plant-based natural antibiotics. This demand has led to more research-based investigations for natural sources of antimicrobial agents and published reports demonstrating that plant extracts are widely applied in modern medicine, reporting potential activity that may be due to polyphenol compounds. Interestingly, the effects of polyphenols on the sensitivity of bacteria to antibiotics have not been well-studied. Hence, the current review encompasses the prospective applicat...
Source: Medicinal Chemistry - April 8, 2024 Category: Chemistry Authors: Alok Sharma None Anurag Jasleen Kaur Anuradh Kesharwani Vipan Parihar Source Type: research
