Characteristics of metabolic stability and the cell permeability of 2 ‐pyrimidynyl‐piperazinyl‐alkyl derivatives of 1H‐imidazo[2,1‐f]purine‐2,4(3H,8H)‐dione with antidepressant‐ and anxiolytic‐like activity
This article is protected by copyright. All rights reserved. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 13, 2018 Category: Biology Authors: Agnieszka Zag órska, Anna Partyka, Adam Bucki, Marcin Kołaczkowski, Magdalena Jastrzębska‐Więsek, Anna Czopek, Agata Siwek, Monika Głuch‐Lutwin, Marek Bednarski, Marek Bajda, Jakub Jończyk, Kamil Piska, Paulina Koczurkiewicz, Anna W Tags: Research Article Source Type: research

3D perspective into MIA ‐QSAR: A case for anti‐HCV agents
This study reports an attempt to incorporate conformational information in MIA ‐QSAR to become it a three‐dimensional method. The geometry optimization and alignment steps to generate 2D‐image projections from 3D‐chemical structures was successful, but the QSAR model obtained traditionally was better. Because image superposition of the flexible structures does not allo w a perfectly aligned perspective of the congeneric moieties, it follows that connectivity of atoms, as well as atomic properties, are still more encoding molecular descriptors in MIA‐QSAR than conformational fingerprints. AbstractQuantitative Stru...
Source: Chemical Biology and Drug Design - November 9, 2018 Category: Biology Authors: Joyce K. Dar é, Teodorico C. Ramalho, Matheus P. Freitas Tags: Special Issue Article Source Type: research

Natural Compounds with xanthine oxidase inhibitory activity: A review
This article is protected by copyright. All rights reserved. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 7, 2018 Category: Biology Authors: Arshad Mehmood, Muhammad Ishaq, Lei Zhao, Bushra Safdar, Ashfaq ‐ur Rehman, Masooma Munir, Ali Raza, Muhammad Nadeem, Waheed Iqbal, Chengtao Wang Tags: Review Source Type: research

Click chemistry ‐based synthesis and cytotoxic activity evaluation of 4α‐triazole acetate podophyllotoxin derivatives
Chemical Biology&Drug Design,Volume 0, Issue ja, -Not available-. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 5, 2018 Category: Biology Authors: Wei Hou, Guanjun Zhang, Zhi Luo, Lin Su, Hongtao Xu Source Type: research

One pot multi component synthesis of functionalized spiropyridine and pyrido[2,3 ‐d]pyrimidine scaffolds and their potent in‐vitro anti‐inflammatory and anti‐oxidant investigations
Chemical Biology&Drug Design,Volume 0, Issue ja, -Not available-. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 5, 2018 Category: Biology Authors: Mallu Lavanya, Indira Viswambaran Asharani, Dhakshanamurthy Thirumalai Source Type: research

Design and Synthesis of 2 ‐Phenyl Benzimidazole Derivatives as VEGFR‐2 Inhibitors with Anti‐Breast Cancer Activity
Chemical Biology&Drug Design,Volume 0, Issue ja, -Not available-. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 5, 2018 Category: Biology Authors: Amany S. Mostafa, Rania M. Gomaa, Mohammad A. Elmorsy Source Type: research

Design and Synthesis of 2 ‐Phenyl Benzimidazole Derivatives as VEGFR‐2 Inhibitors with Anti‐Breast Cancer Activity
This article is protected by copyright. All rights reserved. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 4, 2018 Category: Biology Authors: Amany S. Mostafa, Rania M. Gomaa, Mohammad A. Elmorsy Tags: Research Article Source Type: research

One pot multi component synthesis of functionalized spiropyridine and pyrido[2,3 ‐d]pyrimidine scaffolds and their potent in‐vitro anti‐inflammatory and anti‐oxidant investigations
This article is protected by copyright. All rights reserved. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 4, 2018 Category: Biology Authors: Mallu Lavanya, Indira Viswambaran Asharani, Dhakshanamurthy Thirumalai Tags: Research Article Source Type: research

Click chemistry ‐based synthesis and cytotoxic activity evaluation of 4α‐triazole acetate podophyllotoxin derivatives
This article is protected by copyright. All rights reserved. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 4, 2018 Category: Biology Authors: Wei Hou, Guanjun Zhang, Zhi Luo, Lin Su, Hongtao Xu Tags: Research Article Source Type: research

Bitterless guaifenesin prodrugs —design, synthesis, characterization, in vitro kinetics, and bitterness studies
A number of novel bitterless ester guaifenesin prodrugs were designed, synthesized, and characterized. The prodrugs have shown sufficient stability at neutral pH values and rapid release under low pH conditions (stomach). Using bitter taste receptor assays, it was confirmed that the most promiscuous human bitter taste receptor responsible for the bitter perception of many drugs, the TAS2R14, is not activated by some of the prodrugs. We conclude that our approach could be used to mask the bitterness of other similar drugs. AbstractA respected number of drugs suffer from bitter taste which results in patient incompliance. Wi...
Source: Chemical Biology and Drug Design - November 2, 2018 Category: Biology Authors: Amin Thawabteh, Filomena Lelario, Laura Scrano, Sabino A. Bufo, Stefanie Nowak, Maik Behrens, Antonella Di Pizio, Masha Y. Niv, Rafik Karaman Tags: RESEARCH ARTICLE Source Type: research

Bitterless guaifenesin prodrugs —design, synthesis, characterization, in vitro kinetics, and bitterness studies
Chemical Biology&Drug Design, EarlyView. (Source: Chemical Biology and Drug Design)
Source: Chemical Biology and Drug Design - November 2, 2018 Category: Biology Authors: Amin Thawabteh, Filomena Lelario, Laura Scrano, Sabino A. Bufo, Stefanie Nowak, Maik Behrens, Antonella Di Pizio, Masha Y. Niv, Rafik Karaman Source Type: research