Development of tryptase inhibitors derived from thalidomide

M Tetsuhashi, M Ishikawa, M Hashimoto…

Index: Tetsuhashi, Masashi; Ishikawa, Minoru; Hashimoto, Mariko; Hashimoto, Yuichi; Aoyama, Hiroshi Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 14 p. 5323 - 5338

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Citation Number: 10

Abstract

A novel series of tryptase inhibitors with a N-phenylphthalimide skeleton structurally derived from thalidomide (1) has been developed. Structure–activity relationship studies led to a potent and selective tryptase inhibitor, 2-(4-cyanophenyl) isoindole-1, 3-dione-5-yl 3-(2- aminopyridin-5-yl) propanoate (7), with the IC50 value of 78nM.