Article
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
Journal of medicinal chemistry - 11 Nov 2010
Ali Akbar, Reddy G S Kiran Kumar, Nalam Madhavi N L, Anjum Saima Ghafoor, Cao Hong, Schiffer Celia A, Rana Tariq M
Abstract excerpt
A series of new HIV-1 protease inhibitors with the hydroxyethylamine core and different phenyloxazolidinone P2 ligands were designed and synthesized. Variation of phenyl substitutions at the P2 and P2' moieties significantly affected the binding affinity and antiviral potency of the inhibitors. In general, compounds with 2- and 4-substituted phenyloxazolidinones at P2 exhibited lower binding affinities than...
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