Studies on New Platelet Aggregation Inhibitors 1. Synthesis of 7-Nitro-3,4-dihydroquinoline-2(1H)-one Derivatives.

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  • IYOBE Akira
    Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
  • UCHIDA Masahiko
    Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
  • KAMATA Kouji
    Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
  • HOTEI Yukihiko
    Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
  • KUSAMA Hiroshi
    Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
  • HARADA Hiromu
    Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.

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A series of 6-cyclic aliphatic amino-7-nitro-3, 4-dihydroquinoline-2(1H)-ones were prepared and tested for platelet aggregation inhibitory effect, cardiotonic activity and chronotropic activity. These compounds appeared to show selective inhibitory activity against platelet aggregation. Among them, 6-(4-ethoxycarbonylpiperidino)-7-nitro-3, 4-dihydroquinoline-2(1H)-one (22f) showed the most potent inhibitory activity and high selectivity. A divergent synthetic route to 6-cyclic aliphatic amino-7-nitro-3, 4-dihydroquinoline-2(1H)-one derivatives has also been investigated.

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