Development of tryptase inhibitors derived from thalidomide

作者：Tetsuhashi Masashi; Ishikawa Minoru; Hashimoto Mariko; Hashimoto Yuichi; Aoyama Hiroshi^*

来源：Bioorganic & Medicinal Chemistry, 2010, 18(14): 5323-5338.

DOI：10.1016/j.bmc.2010.05.037

• Tryptase
• Serine protease
• Thalidomide
• Phthalimide
• Inhibitor

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 IC(50) value of 78 nM.

• 出版日期2010-7-15