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576307 
Journal Article 
Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate 
Mowbray, CE; Burt, C; Corbau, R; Gayton, S; Hawes, M; Perros, M; Tran, I; Price, DA; Quinton, FJ; Selby, MD; Stupple, PA; Webster, R; Wood, A 
2009 
Yes 
Bioorganic & Medicinal Chemistry Letters
ISSN: 0960-894X
EISSN: 1464-3405 
19 
20 
5857-5860 
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. 
HIV; RT; Reverse transcriptase; NNRTI; Lersivirine; AIDS