β-Methanesulfonyl-L-valine as a novel, unnatural amino acid surrogate for P2 in the design of HIV protease inhibitors.

Structure-based design of achiral, nonpe

Structure-based design of achiral, nonpeptidic hydroxybenzamide as a novel P2/P2′ replacement for the symmetry-based HIV protease inhibitors

✍ Ramnarayan S. Randad; Lucyna Lubkowska; Abelardo M. Silva; Diego M.A. Guerin; Se 📂 Article 📅 1996 🏛 Elsevier Science 🌐 English ⚖ 737 KB

A combination of structure-activity studies, kinetic analysis, X-ray crystallographic analysis, and modeling were employed in the design of a novel series of HIV-1 protease (HIV PR) inhibitors. The crystal structure of a complex of HIV PR with SRSS-2,5-bis[N-(tert-butyloxycarbonyl)amino]-3,4-dihydro