Naginbhai M. Patel

The synthesis of novel HIV-protease inhibitors

The syntheses, enzyme inhibition and antiviral activity of potent HIV-protease inhibitors containing novel beta-hydroxy ether and thioethers based on the transition state mimetic concept are discussed.

A concise, general enantioselective synthetic route to 2(R)- and 2(S)-[1′(S)-azido-2-phenylethyl]oxirane and related epoxides

The title oxiranes were constructed in > 95% enantiomeric excess (e.e.) utilizing a Sharpless asymmetric epoxidation followed by regioselective azide displacement with [Ti(OPri)2(N3)2] as the key steps.

Novel HIV- protease inhibitors containing β-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand

Studies involving modifications to the P3 position of previously described HIV-protease inhibitors containing beta-hydroxyether and thioether dipeptide isostere replacements led to the discovery of pseudopeptides 8o and 8p with improved antiviral activities.