Studies on 2-Oxoquinoline Derivatives as Blood Platelet Aggregation Inhibitors. III. N-Cyclohexyl-N-(2-hydroxyethyl)-4-(1, 2-dihydro-2-oxo-6-quinolyloxy)-butyramide and Related Compounds

Abstract

A series of N, N-disubstituted-ω-(1, 2-dihydro-2-oxoquinolyloxy) alkanecarboxamides was synthesized and tested for inhibitory activity towards collagen- and ADP-induced aggregation of rabbit blood platelet in vitro. These compounds were prepared by the reaction of ω-(1, 2-dihydro-2-oxoquinolyloxy) alkanoic acid and various amines by the mixed anhydride method. Among them, N-cyclohexyl-N-(2-hydroxyethyl)-4-(1, 2-dihydro-2-oxo-6-quinolyloxy) butyramide (IVa₁) was found to have the most potent inhibitory activity. The structure-activity relationships are discussed.