Koga Y, Kihara Y, Okada M, Inoue Y, Tochizawa S, Toga K, Tachibana K, Kimura Y, Nishi T, Hidaka H
3rd Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd., Japan.
Bioorg Med Chem Lett. 1998 Jun 16;8(12):1471-6. doi: 10.1016/s0960-894x(98)00246-7.
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.
为了寻找抗动脉狭窄药物，合成了一系列2(1H)-喹啉酮衍生物，并对其抗血栓形成活性和抗增生活性进行了评估。从该系列化合物中，通过平衡抗血栓形成和抗增生的疗效，选择了(-)-6-[3-[3-环丙基-3-[(1R,2R)-2-羟基环己基]脲基]丙氧基]-2(1H)-喹啉酮(1p，OPC-33509)作为最佳候选药物。
