Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors |
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| Authors: | Dener J M Wang V R Rice K D Gangloff A R Kuo E Y Newcomb W S Putnam D Wong M |
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| Affiliation: | Department of Medicinal Chemistry, Axys Pharmaceuticals, Inc. 180 Kimball Way, South San Francisco, CA 94080, USA. dener@chemrx.com |
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| Abstract: | Truncation of potent and selective dibasic inhibitors afforded monocharged inhibitors of human mast-cell tryptase. Using two classes of analogues as lead structures, several monocharged derivatives were identified with K(i) values ranging from 0.084 to 0.21 microM against the enzyme. |
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