2. Academic Validation
  3. Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2

Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2

  • J Med Chem. 2004 Nov 18;47(24):5923-36. doi: 10.1021/jm040072r.
George A Freeman 1,  C Webster Andrews Iii 3rd,  Andrew L Hopkins,  Gina S Lowell,  Lee T Schaller,  Jill R Cowan,  Stephen S Gonzales,  George W Koszalka,  Richard J Hazen,  Lawrence R Boone,  Rob G Ferris,  Katrina L Creech,  Grace B Roberts,  Steven A Short,  Kurt Weaver,  David J Reynolds,  John Milton,  Jingshan Ren,  David I Stuart,  David K Stammers,  Joseph H Chan
Affiliations

Affiliation

  • 1 GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. [email protected]
PMID: 15537347 DOI: 10.1021/jm040072r
Abstract

HIV-1 nonnucleoside Reverse Transcriptase inhibitors (NNRTIs) are part of the combination therapy currently used to treat HIV Infection. The features of a new NNRTI drug for HIV treatment must include selective potent activity against both wild-type virus as well as against mutant virus that have been selected by use of current antiretroviral treatment regimens. Based on analogy with known HIV-1 NNRTI inhibitors and modeling studies utilizing the X-ray crystal structure of inhibitors bound in the HIV-1 RT, a series of substituted 2-quinolones was synthesized and evaluated as HIV-1 inhibitors.

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