Title of article
Development of tryptase inhibitors derived from thalidomide Original Research Article
Author/Authors
Masashi Tetsuhashi، نويسنده , , Minoru Ishikawa، نويسنده , , Mariko Hashimoto، نويسنده , , Yuichi Hashimoto، نويسنده , , Hiroshi Aoyama، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2010
Pages
16
From page
5323
To page
5338
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.
Keywords
Ceramide , Partial atomic charge , MTT viability assay , Inductive effects , Structure–activity relationship , Resonance , Sphingosine-1-phosphate
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2010
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306733
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