1.
Bioorg Med Chem Lett
; 19(20): 5857-60, 2009 Oct 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19748778
RESUMO
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.