title: Development of tryptase inhibitors derived from thalidomide.
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.
authors.affiliation: Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
authors.forename: Masashi
authors.initials: M
authors.lastname: Tetsuhashi
authors.forename: Minoru
authors.initials: M
authors.lastname: Ishikawa
authors.forename: Mariko
authors.initials: M
authors.lastname: Hashimoto
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Hashimoto
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Aoyama
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D010797:Phthalimides / Q000737:chemistry; D013792:Thalidomide / Q000737:chemistry* / Q000494:pharmacology*; D053802:Tryptases / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D004791:Enzyme Inhibitors; D010797:Phthalimides; D013792:Thalidomide; C037430:N-phenylphthalimide; D053802:Tryptases