Studies on 2-oxoquinoline derivatives as blood platelet aggregation inhibitors. II. 6-(3-(1-Cyclohexyl-5-tetrazolyl)propoxy)-1,2-dihydro-2-oxoquinoline and related compounds.
作者:TAKAO NISHI、FUJIO TABUSA、TATSUYOSHI TANAKA、TAKEFUMI SHIMIZU、TOSHIMI KANBE、YUKIO KIMURA、KAZUYUKI NAKAGAWA
DOI:10.1248/cpb.31.1151
日期:——
A series of ω-(1-substituted-5-tetrazolylalkoxy)-2-oxoquinolines was synthesized and tested for inhibitory activity towards collagen-and adenosine diphosphate (ADP)-induced aggregation of rabbit blood platelets in vitro. These compounds were prepared by the reaction of 1-substituted-5-(ω-chloroalkyl)-tetrazoles and hydroxy-2-oxoquinolines in the presence of a base. Among them, 6-[3-(1-cyclohexyl-5-tetrazolyl)propoxy]-1, 2-dihydro-2-oxoquinoline (IVb) was found to have the most potent inhibitory activity. The structure-activity relationships are discussed.
合成了一系列ω-(1-取代-5-四唑基烷氧基)-2-氧代喹啉类化合物,并在体外测试了它们对胶原蛋白和二磷酸腺苷(ADP)诱导的兔血小板聚集的抑制活性。这些化合物是由 1-取代-5-(ω-氯烷基)-四唑和羟基-2-氧代喹啉在碱存在下反应制备的。其中,6-[3-(1-环己基-5-四唑基)丙氧基]-1, 2-二氢-2-氧代喹啉(IVb)具有最强的抑制活性。本文讨论了其结构-活性关系。