Article
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry - 18 Jun 1998
De Lucca G V, Kim U T, Liang J, Cordova B, Klabe R M, Garber S, Bacheler L T, Lam G N, Wright M R, Logue K A, Erickson-Viitanen S, Ko S S, Trainor G L
Abstract excerpt
Using the structural information gathered from the X-ray structures of various cyclic urea/HIVPR complexes, we designed and synthesized many nonsymmetrical P2/P2'-substituted cyclic urea analogues. Our efforts concentrated on using an indazole as one of the P2 substituents since this group imparted enzyme (Ki) potency as well as translation into excellent antiviral (IC90) potency. The second P2 substituent was...
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