Literature DB >> 18625554

Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase.

Zachary K Sweeney1, Sahaja Acharya, Andrew Briggs, James P Dunn, Todd R Elworthy, Jennifer Fretland, Anthony M Giannetti, Gabrielle Heilek, Yu Li, Ann C Kaiser, Michael Martin, Y David Saito, Mark Smith, Judy M Suh, Steven Swallow, Jeffrey Wu, Julie Q Hang, Amy S Zhou, Klaus Klumpp.   

Abstract

Novel non-nucleoside inhibitors of HIV-RT that contain pyridazinone isosteres were prepared, and a series of triazolinones were found to be potent inhibitors of HIV replication. These compounds were active against several NNRTI-resistant virus strains. Pharmacokinetic studies indicated that inhibitor 7e has good bioavailability in rats. Several fragments of inhibitor 7c were prepared, and the binding of these compounds to HIV-RT was analyzed by surface plasmon resonance spectroscopy.

Entities:  

Mesh:

Substances:

Year:  2008        PMID: 18625554     DOI: 10.1016/j.bmcl.2008.06.080

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Fragment-based inhibitor discovery against β-lactamase.

Authors:  Derek A Nichols; Adam R Renslo; Yu Chen
Journal:  Future Med Chem       Date:  2014-03       Impact factor: 3.808

2.  Molecular docking and 3D-QSAR studies on triazolinone and pyridazinone, non-nucleoside inhibitor of HIV-1 reverse transcriptase.

Authors:  Sree Kanth Sivan; Vijjulatha Manga
Journal:  J Mol Model       Date:  2009-12-15       Impact factor: 1.810

3.  Molecular docking and ligand specificity in fragment-based inhibitor discovery.

Authors:  Yu Chen; Brian K Shoichet
Journal:  Nat Chem Biol       Date:  2009-03-22       Impact factor: 15.040

4.  Microwave assisted synthesis, antifungal activity, and DFT study of some novel triazolinone derivatives.

Authors:  Na-Bo Sun; Jian-Zhong Jin; Fang-Yue He
Journal:  Biomed Res Int       Date:  2015-03-12       Impact factor: 3.411

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.