title: Studies on new platelet aggregation inhibitors 1. Synthesis of 7-nitro-3,4-dihydroquinoline-2(1H)-one derivatives.
abstract: 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.
authors.affiliation: Central Research Laboratories, Kissei Pharmaceutical Co., Ltd., Nagano, Japan. akira_iyobe@pharm.kissei.co.jp
authors.forename: A
authors.initials: A
authors.lastname: Iyobe
authors.forename: M
authors.initials: M
authors.lastname: Uchida
authors.forename: K
authors.initials: K
authors.lastname: Kamata
authors.forename: Y
authors.initials: Y
authors.lastname: Hotei
authors.forename: H
authors.initials: H
authors.lastname: Kusama
authors.forename: H
authors.initials: H
authors.lastname: Harada
mesh_terms: D000107:Acetylation; D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D009200:Myocardial Contraction / Q000187:drug effects; D009574:Nitro Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship
chemical_list: D002316:Cardiotonic Agents; D007202:Indicators and Reagents; D009574:Nitro Compounds; D010975:Platelet Aggregation Inhibitors; D015363:Quinolones