Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)

Zhijian Zhao; Scott E Wolkenberg; Philip E J Sanderson; Meiqing Lu; Vandna Munshi; Gregory Moyer; Meizhen Feng; Anthony V Carella; Linda T Ecto; Lori J Gabryelski; Ming-Tain Lai; Sridar G Prasad; Youwei Yan; Georgia B McGaughey; Michael D Miller; Craig W Lindsley; George D Hartman; Joseph P Vacca; Theresa M Williams

doi:10.1016/j.bmcl.2007.11.085

Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)

Bioorg Med Chem Lett. 2008 Jan 15;18(2):554-9. doi: 10.1016/j.bmcl.2007.11.085. Epub 2007 Nov 28.

Affiliation

¹ Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA. zhijian_zhao@merck.com

PMID: 18083561
DOI: 10.1016/j.bmcl.2007.11.085

Abstract

This Letter describes the design, synthesis, and biological evaluation of novel 3-indole sulfonamides as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) with balanced profiles against common HIV RT mutants K103N and Y181C.

MeSH terms

Crystallography, X-Ray
HIV Reverse Transcriptase / antagonists & inhibitors
HIV Reverse Transcriptase / genetics
Indoles / chemistry*
Models, Molecular
Mutation
Reverse Transcriptase Inhibitors / chemistry
Reverse Transcriptase Inhibitors / pharmacology*
Sulfonamides / chemistry
Sulfonamides / pharmacology*

Substances

Indoles
Reverse Transcriptase Inhibitors
Sulfonamides
reverse transcriptase, Human immunodeficiency virus 1
HIV Reverse Transcriptase