Bioorganic & Medicinal Chemistry 2010-07-15

Development of tryptase inhibitors derived from thalidomide.

Masashi Tetsuhashi, Minoru Ishikawa, Mariko Hashimoto, Yuichi Hashimoto, Hiroshi Aoyama

Index: Bioorg. Med. Chem. 18(14) , 5323-38, (2010)

Full Text: HTML

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 78 nM.Copyright (c) 2010 Elsevier Ltd. All rights reserved.