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

Abstract In order to search for anti-arteriostenotic agents, a series of 2(1 H )-quinolinone derivatives was synthesized and evaluated for anti-thrombotic activity and for anti-hyperplastic activity. From this series, (−)-6-[3-[3-cyclopropyl-3-[(1 R ,2 R )-2-hydroxycyclohexyl]ureido]propoxy]-2(1 H )-quinolinone ( 1p , OPC-33509) was selected as the best candidate by balancing the efficacy on anti-thrombosis and anti-hyperplasia.