Literature DB >> 16499282

Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors.

Lawrence R Boone1.   

Abstract

This review discusses the desired attributes of a next-generation HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) and highlights the properties of compounds currently or recently in clinical development. TMC-125 is currently in phase III clinical trials and on track to become the first NNRTI suitable for use in NNRTI-experienced patients. TMC-278 is structurally related to TMC-125, but is more potent in vitro and has pharmacokinetics suitable for once-daily administration. It is currently undergoing phase II clinical trials. BILR-355 BS, a dipyridodiazepinone compound, is in early phase II clinical trials. It requires ritonavir as a booster and has reduced inhibitory activity against several key NNRTI-resistant HIV-1 strains. Development of the NNRTIs capravirine and GW-695634 has been discontinued because of lack of efficacy and safety issues, respectively.

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Year:  2006        PMID： 16499282

Source DB:  PubMed          Journal:  Curr Opin Investig Drugs        ISSN： 1472-4472


  8 in total

1.  A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.

Authors:  Zhijun Zhang; Wen Xu; Yung-Hyo Koh; Jae Hoon Shim; Jean-Luc Girardet; Li-Tain Yeh; Robert K Hamatake; Zhi Hong
Journal:  Antimicrob Agents Chemother       Date:  2006-11-20       Impact factor: 5.191

2.  Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H.

Authors:  Suhman Chung; Daniel M Himmel; Jian-Kang Jiang; Krzysztof Wojtak; Joseph D Bauman; Jason W Rausch; Jennifer A Wilson; John A Beutler; Craig J Thomas; Eddy Arnold; Stuart F J Le Grice
Journal:  J Med Chem       Date:  2011-06-02       Impact factor: 7.446

3.  Pharmacokinetics of BILR 355 after multiple oral doses coadministered with a low dose of ritonavir.

Authors:  Fenglei Huang; Kristin Drda; Thomas R MacGregor; Joseph Scherer; Lois Rowland; Thuy Nguyen; Charles Ballow; Mark Castles; Patrick Robinson
Journal:  Antimicrob Agents Chemother       Date:  2008-10-27       Impact factor: 5.191

4.  Pharmacokinetic and safety evaluation of BILR 355, a second-generation nonnucleoside reverse transcriptase inhibitor, in healthy volunteers.

Authors:  Fenglei Huang; Michael Koenen-Bergmann; Thomas R Macgregor; Arne Ring; Susan Hattox; Patrick Robinson
Journal:  Antimicrob Agents Chemother       Date:  2008-09-29       Impact factor: 5.191

Review 5.  Non-nucleoside reverse transcriptase inhibitors: a review on pharmacokinetics, pharmacodynamics, safety and tolerability.

Authors:  Iris Usach; Virginia Melis; José-Esteban Peris
Journal:  J Int AIDS Soc       Date:  2013-09-04       Impact factor: 5.396

6.  Microwave-Assisted Expeditious Synthesis of 2-Alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines Catalyzed by HgCl₂ under Solvent-Free Conditions as Potential Anti-HIV-1 Agents.

Authors:  Zhiping Che; Yuee Tian; Shengming Liu; Jia Jiang; Mei Hu; Genqiang Chen
Journal:  Molecules       Date:  2018-11-10       Impact factor: 4.411

7.  In silico studies of diarylpyridine derivatives as novel HIV-1 NNRTIs using docking-based 3D-QSAR, molecular dynamics, and pharmacophore modeling approaches.

Authors:  Youlan Wan; Yafeng Tian; Wenjie Wang; Shuangxi Gu; Xiulian Ju; Genyan Liu
Journal:  RSC Adv       Date:  2018-12-05       Impact factor: 4.036

Review 8.  Structural biology in antiviral drug discovery.

Authors:  Marcella Bassetto; Alberto Massarotti; Antonio Coluccia; Andrea Brancale
Journal:  Curr Opin Pharmacol       Date:  2016-09-06       Impact factor: 5.547
  8 in total

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