title: Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.
abstract: An efficient solid-phase synthesis of benzisothiazolone-1,1-dioxide-based serine protease inhibitors involving alkylation of carboxylic acids with N-(bromomethyl)benzisothiazolone-1,1-dioxide has been developed. An example using this procedure for preparation of a library of human mast cell tryptase inhibitors is described.
authors: Bristol-Myers Squibb Pharmaceutical Research Institute, Department of Chemistry, Wallingford, CT 06492, USA.
authors: K L
authors: KL
authors: Yu
authors: R
authors: R
authors: Civiello
authors: D G
authors: DG
authors: Roberts
authors: S M
authors: SM
authors: Seiler
authors: N A
authors: NA
authors: Meanwell
mesh_terms: D053818:Chymases; D006801:Humans; D008407:Mast Cells / Q000187:drug effects / Q000201:enzymology; D012697:Serine Endopeptidases / Q000378:metabolism; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D053802:Tryptases
chemical_list: D015842:Serine Proteinase Inhibitors; D013844:Thiazoles; D012697:Serine Endopeptidases; C083294:chymase 2; D053818:Chymases; D053802:Tryptases; C015699:1,2-benzisothiazoline-3-one