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
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, WP14-3, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, USA. [email protected]
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.