Literature DB >> 19666220

Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Xingtao Tian1, Bingjie Qin, Hong Lu, Weihong Lai, Shibo Jiang, Kuo-Hsiung Lee, Chin Ho Chen, Lan Xie.   

Abstract

Two series (4 and 5) of diarylpyridine derivatives were designed, synthesized, and evaluated for anti-HIV-1 activity. The most promising compound, 5e, inhibited HIV-1 IIIB, NL4-3, and RTMDR1 with low nanomolar EC50 values and selectivity indexes of >10,000. The results of this study indicate that diarylpyridine can be used as a novel scaffold to derive a new class of potent NNRTIs, active against both wild-type and drug-resistant HIV-1 strains.

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Year:  2009        PMID： 19666220      PMCID： PMC2770631          DOI： 10.1016/j.bmcl.2009.07.080

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


  13 in total

1.  Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK).

Authors:  Lan Xie; Huan-Fang Guo; Hong Lu; Xiao-Mei Zhuang; An-Ming Zhang; Gang Wu; Jin-Xiu Ruan; Ting Zhou; Donglei Yu; Keduo Qian; Kuo-Hsiung Lee; Shibo Jiang
Journal:  J Med Chem       Date:  2008-12-25       Impact factor: 7.446

Review 2.  From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Authors:  Bart L De Corte
Journal:  J Med Chem       Date:  2005-03-24       Impact factor: 7.446

3.  Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.

Authors:  D W Ludovici; B L De Corte; M J Kukla; H Ye; C Y Ho; M A Lichtenstein; R W Kavash; K Andries; M P de Béthune; H Azijn; R Pauwels; P J Lewi; J Heeres; L M Koymans; M R de Jonge; K J Van Aken; F F Daeyaert; K Das; E Arnold; P A Janssen
Journal:  Bioorg Med Chem Lett       Date:  2001-09-03       Impact factor: 2.823

4.  TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1.

Authors:  Koen Andries; Hilde Azijn; Theo Thielemans; Donald Ludovici; Michael Kukla; Jan Heeres; Paul Janssen; Bart De Corte; Johan Vingerhoets; Rudi Pauwels; Marie-Pierre de Béthune
Journal:  Antimicrob Agents Chemother       Date:  2004-12       Impact factor: 5.191

Review 5.  Crystallography and the design of anti-AIDS drugs: conformational flexibility and positional adaptability are important in the design of non-nucleoside HIV-1 reverse transcriptase inhibitors.

Authors:  Kalyan Das; Paul J Lewi; Stephen H Hughes; Eddy Arnold
Journal:  Prog Biophys Mol Biol       Date:  2005-06       Impact factor: 3.667

6.  A series of diaryltriazines and diarylpyrimidines are highly potent nonnucleoside reverse transcriptase inhibitors with possible applications as microbicides.

Authors:  Yven Van Herrewege; Guido Vanham; Jo Michiels; Katrien Fransen; Luc Kestens; Koen Andries; Paul Janssen; Paul Lewi
Journal:  Antimicrob Agents Chemother       Date:  2004-10       Impact factor: 5.191

Review 7.  New non-nucleoside reverse transcriptase inhibitors (NNRTIs) in development for the treatment of HIV infections.

Authors:  Rudi Pauwels
Journal:  Curr Opin Pharmacol       Date:  2004-10       Impact factor: 5.547

8.  Convergent combination therapy can select viable multidrug-resistant HIV-1 in vitro.

Authors:  B A Larder; P Kellam; S D Kemp
Journal:  Nature       Date:  1993-09-30       Impact factor: 49.962

9.  High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations.

Authors:  Kalyan Das; Joseph D Bauman; Arthur D Clark; Yulia V Frenkel; Paul J Lewi; Aaron J Shatkin; Stephen H Hughes; Eddy Arnold
Journal:  Proc Natl Acad Sci U S A       Date:  2008-01-29       Impact factor: 11.205

Review 10.  Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV.

Authors:  Erik De Clercq
Journal:  Int J Antimicrob Agents       Date:  2008-12-23       Impact factor: 5.283
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  5 in total

1.  Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.

Authors:  Bingjie Qin; Xingkai Jiang; Hong Lu; Xingtao Tian; Florent Barbault; Li Huang; Keduo Qian; Chin-Ho Chen; Rong Huang; Shibo Jiang; Kuo-Hsiung Lee; Lan Xie
Journal:  J Med Chem       Date:  2010-07-08       Impact factor: 7.446

2.  Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

Authors:  Xingtao Tian; Bingjie Qin; Zhiyuan Wu; Xiaofeng Wang; Hong Lu; Susan L Morris-Natschke; Chin Ho Chen; Shibo Jiang; Kuo-Hsiung Lee; Lan Xie
Journal:  J Med Chem       Date:  2010-11-04       Impact factor: 7.446

3.  Optimization of the antiviral potency and lipophilicity of halogenated 2,6-diarylpyridinamines as a novel class of HIV-1 NNRTIS.

Authors:  Zhi-Yuan Wu; Na Liu; Bingjie Qin; Li Huang; Fei Yu; Keduo Qian; Susan L Morris-Natschke; Shibo Jiang; Chin Ho Chen; Kuo-Hsiung Lee; Lan Xie
Journal:  ChemMedChem       Date:  2014-06-04       Impact factor: 3.466

4.  Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.

Authors:  Na Liu; Lei Wei; Li Huang; Fei Yu; Weifan Zheng; Bingjie Qin; Dong-Qin Zhu; Susan L Morris-Natschke; Shibo Jiang; Chin-Ho Chen; Kuo-Hsiung Lee; Lan Xie
Journal:  J Med Chem       Date:  2016-04-12       Impact factor: 7.446

5.  Combining New Non-Nucleoside Reverse Transcriptase Inhibitors (RTIs) with AZT Results in Strong Synergism against Multi-RTI-Resistant HIV-1 Strains.

Authors:  Fei Yu; Wen Li; Lili Wang; Yu Dai; Xin Lu; Qian Wang; Lan Xie; Shibo Jiang
Journal:  Molecules       Date:  2018-07-02       Impact factor: 4.411
  5 in total

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