Novel 1,5-Diphenylpyrazole Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted Derivatives
Genin, Michael J.;Biles, Carolyn;Keiser, Barb J.;Poppe, Susan M.;Swaney, Steven M.;Tarpley, W. Gary;Yagi, Yoshihiko;Romero, Donna L.
Journal of medicinal chemistry2000Vol. 43pp. 1034-1040
422
genin2000novel
Abstract
Through computationally directed broad screening, a novel 1,5-diphenylpyrazole (DPP) class of HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) has been discovered. Compound 2 (PNU-32945) was found to have good activity versus wild-type (IC50