Rational design of irreversible, pseudo-C2-symmetric hiv-1 protease inhibitors

Bioorganic & Medicinal Chemistry Letters
1995.0

Abstract

Pseudo-C2-symmetric irreversible inhibitors of HIV-1 protease containing cisepoxide were designed, synthesized, and kinetically characterized. Introduction of a Gly residue into P1' of the inactivators yielded strong time-dependent irreversible ones with kina/Ki ranging from 1.5×10⁸ to 3.4×10⁵ M⁻¹min⁻¹.

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