title: Total synthesis of human chymase inhibitor methyllinderone and structure--activity relationships of its derivatives.
abstract: Total synthesis of human chymase inhibitor methyllinderone has been achieved in only four steps with an overall yield of 21% from dimethyl squarate. We developed an efficient synthetic method for obtaining methyllinderone derivatives and found the active compound. In addition, we propose the inhibition mechanism of the active compound against human chymase using calculations.
authors: Shionogi Research Laboratories, Shionogi & Co., Ltd., Fukushima-ku, 553-0002, Osaka, Japan. yasunori.aoyama@shionogi.co.jp
authors: Y
authors: Y
authors: Aoyama
authors: T
authors: T
authors: Konoike
authors: A
authors: A
authors: Kanda
authors: N
authors: N
authors: Naya
authors: M
authors: M
authors: Nakajima
mesh_terms: D000475:Alkenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D053818:Chymases; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D012697:Serine Endopeptidases / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000475:Alkenes; D003517:Cyclopentanes; D004791:Enzyme Inhibitors; C434647:methyllinderone; D012697:Serine Endopeptidases; D053818:Chymases