Literature DB >> 16480871

Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands.

Arun K Ghosh1, Gary Schiltz, Ramu Sridhar Perali, Sofiya Leshchenko, Stephanie Kay, D Eric Walters, Yasuhiro Koh, Kenji Maeda, Hiroaki Mitsuya.   

Abstract

A series of novel oxyindole-derived HIV-1 protease inhibitors were designed and synthesized based upon our X-ray crystal structure of inhibitor 2 (TMC-114) bound to HIV-1 protease. The effects of substituents, spirocyclic rings, and ring sizes have been investigated. A number of inhibitors exhibited low nanomolar inhibitory potencies against HIV protease.

Entities:  

Mesh:

Substances:

Year:  2006        PMID: 16480871     DOI: 10.1016/j.bmcl.2006.01.011

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


  8 in total

Review 1.  Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS.

Authors:  Arun K Ghosh; Heather L Osswald; Gary Prato
Journal:  J Med Chem       Date:  2016-01-22       Impact factor: 7.446

Review 2.  Tetrahydrofuran, tetrahydropyran, triazoles and related heterocyclic derivatives as HIV protease inhibitors.

Authors:  Arun K Ghosh; David D Anderson
Journal:  Future Med Chem       Date:  2011-07       Impact factor: 3.808

3.  A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.

Authors:  Masayuki Amano; Yasuhiro Koh; Debananda Das; Jianfeng Li; Sofiya Leschenko; Yuan-Fang Wang; Peter I Boross; Irene T Weber; Arun K Ghosh; Hiroaki Mitsuya
Journal:  Antimicrob Agents Chemother       Date:  2007-03-19       Impact factor: 5.191

4.  Hybrid-genetic algorithm based descriptor optimization and QSAR models for predicting the biological activity of Tipranavir analogs for HIV protease inhibition.

Authors:  A Srinivas Reddy; Sunil Kumar; Rajni Garg
Journal:  J Mol Graph Model       Date:  2010-03-24       Impact factor: 2.518

5.  Enantioselective Synthesis of Spiro[cyclohexane-1,3'-indolin]-2'-ones Containing Multiple Stereocenters via Organocatalytic Michael/Aldol Cascade Reactions.

Authors:  Arun K Ghosh; Bing Zhou
Journal:  Tetrahedron Lett       Date:  2013-05-08       Impact factor: 2.415

Review 6.  Therapeutic Potential of Spirooxindoles as Antiviral Agents.

Authors:  Na Ye; Haiying Chen; Eric A Wold; Pei-Yong Shi; Jia Zhou
Journal:  ACS Infect Dis       Date:  2016-05-05       Impact factor: 5.084

7.  1,3-Dipolar cycloaddition of isatin N,N'-cyclic azomethine imines with α,β-unsaturated aldehydes catalyzed by DBU in water.

Authors:  Zhan-Yong Wang; Ting Yang; Rongxiang Chen; Xueji Ma; Huan Liu; Kai-Kai Wang
Journal:  RSC Adv       Date:  2020-06-25       Impact factor: 4.036

8.  Iodide/H₂O₂ Catalyzed Intramolecular Oxidative Amination for the Synthesis of 3,2'-Pyrrolidinyl Spirooxindoles.

Authors:  Yu-Ting Gao; Xiao-Yang Jin; Qi Liu; An-Di Liu; Liang Cheng; Dong Wang; Li Liu
Journal:  Molecules       Date:  2018-09-05       Impact factor: 4.411

  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.