Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase

…, Y Luo, HK Lim, R Vaz, S Rebello, S Maignan…

Index: Hopkins, Corey R.; Czekaj, Mark; Kaye, Steven S.; Gao, Zhongli; Pribish, James; Pauls, Henry; Liang, Guyan; Sides, Keith; Cramer, Dona; Cairns, Jennifer; Luo, Yongyi; Lim, Heng-Keang; Vaz, Roy; Rebello, Sam; Maignan, Sebastian; Dupuy, Alain; Mathieu, Magali; Levell, Julian Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 11 p. 2734 - 2737

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Citation Number: 29

Abstract

A new series of novel mast cell tryptase inhibitors is reported, which features the use of an indole structure as the hydrophobic substituent on a m-benzylaminepiperidine template. The best members of this series display good in vitro activity and excellent selectivity against other serine proteases.