2. Academic Validation
  3. The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations

The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2959-66. doi: 10.1016/j.bmcl.2008.03.064.
Thomas J Tucker 1,  Sandeep Saggar,  John T Sisko,  Robert M Tynebor,  Theresa M Williams,  Peter J Felock,  Jessica A Flynn,  Ming-Tain Lai,  Yuexia Liang,  Georgia McGaughey,  Meiquing Liu,  Mike Miller,  Gregory Moyer,  Vandna Munshi,  Rebecca Perlow-Poehnelt,  Sridhar Prasad,  Rosa Sanchez,  Maricel Torrent,  Joseph P Vacca,  Bang-Lin Wan,  Youwei Yan
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, WP14-3, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, USA. tom_tucker@merck.com
PMID: 18396399 DOI: 10.1016/j.bmcl.2008.03.064
Abstract

Using a combination of traditional Medicinal Chemistry/SAR analysis, crystallography, and molecular modeling, we have designed and synthesized a series of novel, highly potent NNRTIs that possess broad Antiviral activity against a number of key clinical mutations.

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