Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality

J M Dener; K D Rice; W S Newcomb; V R Wang; W B Young; A R Gangloff; E Y Kuo; L Cregar; D Putnam; M Wong

doi:10.1016/s0960-894x(01)00254-2

Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1629-33. doi: 10.1016/s0960-894x(01)00254-2.

Authors

J M Dener¹, K D Rice, W S Newcomb, V R Wang, W B Young, A R Gangloff, E Y Kuo, L Cregar, D Putnam, M Wong

Affiliation

¹ Departments of Medicinal Chemistry, Biochemistry, and Enzymology, Axys Pharmaceuticals, Inc., 180 Kimball Way, South 94080, San Francisco, CA, USA. dener@chemrx.com

PMID: 11425524
DOI: 10.1016/s0960-894x(01)00254-2

Abstract

A survey of charged groups and linkers for a series of symmetrical and unsymmetrical dibasic inhibitors is described, leading to several classes of potent and selective inhibitors. In particular, the benzamidine functionality was identified as the most potent charged group investigated.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzamidines / chemistry*
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Humans
Mast Cells / enzymology*
Serine Endopeptidases / drug effects*
Structure-Activity Relationship
Tryptases

Substances

Benzamidines
Enzyme Inhibitors
Serine Endopeptidases
Tryptases