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. 2009 Oct 15;19(20):5857-60.
doi: 10.1016/j.bmcl.2009.08.080. Epub 2009 Aug 27.

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

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

Charles E Mowbray et al. Bioorg Med Chem Lett. .

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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