Use of heteroatom-containing small cyclic compounds for enzyme inhibitor design

Abstract

Varied mode of inhibitors for carboxypeptidase A were designed using heteroatom-containing small rings which interact with the catalytic center to modify it covalently. Substrate analogs having an oxirane ring and those having 2-oxo-1,3-oxazolidine moiety inhibited the enzyme irreversibly, but those bearing β-lactam ring were shown to be reversible competitive inhibitors.