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Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.

Authors
  • Su, Dai-Shi
  • Lim, John J
  • Tinney, Elizabeth
  • Wan, Bang-Lin
  • Young, Mary Beth
  • Anderson, Kenneth D
  • Rudd, Deanne
  • Munshi, Vandna
  • Bahnck, Carolyn
  • Felock, Peter J
  • Lu, Meiquing
  • Lai, Ming-Tain
  • Touch, Sinoeun
  • Moyer, Gregory
  • DiStefano, Daniel J
  • Flynn, Jessica A
  • Liang, Yuexia
  • Sanchez, Rosa
  • Perlow-Poehnelt, Rebecca
  • Miller, Mike
  • And 3 more
Type
Published Article
Journal
Journal of Medicinal Chemistry
Publisher
American Chemical Society
Publication Date
Nov 26, 2009
Volume
52
Issue
22
Pages
7163–7169
Identifiers
DOI: 10.1021/jm901230r
PMID: 19883100
Source
Medline
License
Unknown

Abstract

Biaryl ethers were recently reported as potent NNRTIs. Herein we disclose a detailed SAR study that led to the biaryl ether 6. This compound possessed excellent potency against WT RT and key clinically observed RT mutants and had an excellent pharmacokinetic profile in rats, dogs, and rhesus macaques. The compound also exhibited a clean safety profile in preclinical safety studies.

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