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

…, R Corbau, S Gayton, M Hawes, M Perros, I Tran…

Index: Mowbray, Charles E.; Burt, Catherine; Corbau, Romuald; Gayton, Simon; Hawes, Michael; Perros, Manos; Tran, Isabelle; Price, David A.; Quinton, Faye J.; Selby, Matthew D.; Stupple, Paul A.; Webster, Rob; Wood, Anthony Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 20 p. 5857 - 5860

Full Text: HTML

Citation Number: 58

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.