Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors

Abstract 3-Benzylazetidine-2-one derivatives were designed and evaluated as a novel series of chymase inhibitors. Structure–activity relationship studies of 3-benzylazetidine-2-ones led to compounds 23 , which exhibited 3.1 nM inhibition of human chymase and enhancement of stability in human plasma ( t 1/2 6 h).