title: 2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.
abstract: In order to search for anti-arteriostenotic agents, a series of 2(1H)-quinolinone derivatives was synthesized and evaluated for anti-thrombotic activity and for anti-hyperplastic activity. From this series, (-)-6-[3-[3-cyclopropyl-3-[(1R,2R)-2-hydroxycyclohexyl]ureido]propoxy]-2 (1H)-quinolinone (1p, OPC-33509) was selected as the best candidate by balancing the efficacy on anti-thrombosis and anti-hyperplasia.
authors.affiliation: 3rd Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd., Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Koga
authors.forename: Y
authors.initials: Y
authors.lastname: Kihara
authors.forename: M
authors.initials: M
authors.lastname: Okada
authors.forename: Y
authors.initials: Y
authors.lastname: Inoue
authors.forename: S
authors.initials: S
authors.lastname: Tochizawa
authors.forename: K
authors.initials: K
authors.lastname: Toga
authors.forename: K
authors.initials: K
authors.lastname: Tachibana
authors.forename: Y
authors.initials: Y
authors.lastname: Kimura
authors.forename: T
authors.initials: T
authors.lastname: Nishi
authors.forename: H
authors.initials: H
authors.lastname: Hidaka
mesh_terms: D000818:Animals; D001161:Arteriosclerosis / Q000188:drug therapy*; D000077407:Cilostazol; D006965:Hyperplasia; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D015363:Quinolones / Q000494:pharmacology; D011817:Rabbits; D013777:Tetrazoles / Q000494:pharmacology; D013927:Thrombosis / Q000188:drug therapy*; D014508:Urea / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D010975:Platelet Aggregation Inhibitors; D011804:Quinolines; D015363:Quinolones; D013777:Tetrazoles; C021294:cilostamide; D014508:Urea; C116725:OPC 33509; D000077407:Cilostazol