2. Academic Validation
  3. Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate

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

Affiliation

  • 1 Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK. Charles.Mowbray@Pfizer.Com
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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