Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate

  • Bioorg Med Chem Lett. 2009 Oct 15;19(20):5857-60. doi: 10.1016/j.bmcl.2009.08.080.
Charles E Mowbray  1 ,  Catherine Burt ,  Romuald Corbau ,  Simon Gayton ,  Michael Hawes ,  Manos Perros ,  Isabelle Tran ,  David A Price ,  Faye J Quinton ,  Matthew D Selby ,  Paul A Stupple ,  Rob Webster ,  Anthony Wood
Affiliations
  • 1. Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK. [email protected]
PMID: 19748778 DOI: 10.1016/j.bmcl.2009.08.080
Abstract

We prepared three discreet cohorts of potent non-nucleoside HIV Reverse Transcriptase inhibitors (NNRTIs) based on the recently reported 3-cyanophenoxypyrazole lead 3. Several of these compounds displayed very promising anti-HIV activity in vitro, safety, pharmacokinetic and pharmaceutical profiles. We describe our analysis and conclusions leading to the selection of alcohol 5 (UK-453,061, lersivirine) for clinical development.

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