Literature DB >> 11527703

Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).

D W Ludovici1, M J Kukla, P G Grous, S Krishnan, K Andries, M P de Béthune, H Azijn, R Pauwels, E De Clercq, E Arnold, P A Janssen.   

Abstract

Stemming from work on a previous clinical candidate, loviride, and other alpha-APA derivatives, a new series of potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been synthesized. The ITU analogues, which contain a unique diarylated imidoyl thiourea, are very active in inhibiting both wild-type and clinically important mutant strains of HIV-1.

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Year:  2001        PMID： 11527703     DOI： 10.1016/s0960-894x(01)00410-3

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


  8 in total

1.  On the detection of multiple-binding modes of ligands to proteins, from biological, structural, and modeling data.

Authors:  Paul J Lewi; Marc de Jonge; Frits Daeyaert; Luc Koymans; Maarten Vinkers; Jan Heeres; Paul A J Janssen; Eddy Arnold; Kalyan Das; Art D Clark; Stephen H Hughes; Paul L Boyer; Marie-Pierre de Béthune; Rudi Pauwels; Koen Andries; Mike Kukla; Donald Ludovici; Bart De Corte; Robert Kavash; Chih Ho; Paul J Lewis
Journal:  J Comput Aided Mol Des       Date:  2003 Feb-Apr       Impact factor: 3.686

2.  Antiviral drug resistance and the need for development of new HIV-1 reverse transcriptase inhibitors.

Authors:  Eugene L Asahchop; Mark A Wainberg; Richard D Sloan; Cécile L Tremblay
Journal:  Antimicrob Agents Chemother       Date:  2012-06-25       Impact factor: 5.191

3.  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

4.  The phenylmethylthiazolylthiourea nonnucleoside reverse transcriptase (RT) inhibitor MSK-076 selects for a resistance mutation in the active site of human immunodeficiency virus type 2 RT.

Authors:  Joeri Auwerx; Miguel Stevens; An R Van Rompay; Louise E Bird; Jingshan Ren; Erik De Clercq; Bo Oberg; David K Stammers; Anna Karlsson; Jan Balzarini
Journal:  J Virol       Date:  2004-07       Impact factor: 5.103

5.  Molecular dynamics study of non-nucleoside reverse transcriptase inhibitor 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile (TMC278/rilpivirine) aggregates: correlation between amphiphilic properties of the drug and oral bioavailability.

Authors:  Yulia Volovik Frenkel; Emilio Gallicchio; Kalyan Das; Ronald M Levy; Eddy Arnold
Journal:  J Med Chem       Date:  2009-10-08       Impact factor: 7.446

6.  Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.

Authors:  P Fletcher; S Harman; H Azijn; N Armanasco; P Manlow; D Perumal; M-P de Bethune; J Nuttall; J Romano; R Shattock
Journal:  Antimicrob Agents Chemother       Date:  2008-11-24       Impact factor: 5.191

Review 7.  The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance.

Authors:  Mark A Wainberg
Journal:  Scientifica (Cairo)       Date:  2012-12-31

Review 8.  Approved HIV reverse transcriptase inhibitors in the past decade.

Authors:  Guangdi Li; Yali Wang; Erik De Clercq
Journal:  Acta Pharm Sin B       Date:  2021-11-16       Impact factor: 14.903
  8 in total

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