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
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
Journal title :
Bioorganic and Medicinal Chemistry
