2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.
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.
Koga
Y
Y
3rd Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd., Japan.
Kihara
Y
Y
Okada
M
M
Inoue
Y
Y
Tochizawa
S
S
Toga
K
K
Tachibana
K
K
Kimura
Y
Y
Nishi
T
T
Hidaka
H
H
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
D010975:Platelet Aggregation Inhibitors; D011804:Quinolines; D015363:Quinolones; D013777:Tetrazoles; C021294:cilostamide; D014508:Urea; C116725:OPC 33509; D000077407:Cilostazol