Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate

Charles E. Mowbray, 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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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.

Original languageEnglish
Pages (from-to)5857-5860
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number20
DOIs
Publication statusPublished - 15 Oct 2009
Externally publishedYes

Keywords

  • AIDS
  • HIV
  • Lersivirine
  • NNRTI
  • Reverse transcriptase
  • RT

Cite this

Mowbray, C. E., Burt, C., Corbau, R., Gayton, S., Hawes, M., Perros, M., Tran, I., Price, D. A., Quinton, F. J., Selby, M. D., Stupple, P. A., Webster, R., & Wood, A. (2009). Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate. Bioorganic and Medicinal Chemistry Letters, 19(20), 5857-5860. https://doi.org/10.1016/j.bmcl.2009.08.080