Development of tryptase inhibitors derived from thalidomide |
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| Authors: | Masashi Tetsuhashi Minoru Ishikawa Mariko Hashimoto Yuichi Hashimoto Hiroshi Aoyama |
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| Affiliation: | Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan |
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| 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. |
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