2 (1H)-Quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities

…, S Tochizawa, K Toga, K Tachibana, Y Kimura…

Index: Koga, Yasuo; Kihara, Yoshito; Okada, Minoru; Inoue, Yoshihiro; Tochizawa, Shirou; Toga, Kazuyuki; Tachibana, Kazue; Kimura, Yukio; Nishi, Takao; Hidaka, Hiroyoshi Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 12 p. 1471 - 1476

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Citation Number: 26

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.