doi: 10.1016/j.bmc.2010.05.037.
Epub 2010 Jun 1.
Development of tryptase inhibitors derived from thalidomide
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- PMID: 20561792
- DOI: 10.1016/j.bmc.2010.05.037
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Development of tryptase inhibitors derived from thalidomide
Bioorg Med Chem.
.
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.
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