Various ω-cycloalkyl-2-oxoalkyl arenesulfonates were synthesized and evaluated for esterase-and chymotrypsin-inhibitory activities and hypolipidemic activity. Among the tested compounds, 2-oxoalkyl arenesulfonates (4, 8 and 13) having a cyclohexyl substituent at the terminus of the alkyl chain exhibited considerable esterase-inhibitory activity, and several compounds among 4 and 8 also exhibited potent hypolipidemic action. The structure-activity relationships of these compounds are discussed.
多种ω-环烷基-2-氧代烷基芳
磺酸酯被合成,并评估了其
酯酶和胰凝乳
蛋白酶抑制活性以及降血脂活性。在测试的化合物中,具有烷基链末端环己基取代的2-氧代烷基芳
磺酸酯(4、8和13)表现出显著的
酯酶抑制活性,而4和8中的几种化合物还显示出强大的降血脂作用。本文讨论了这些化合物的结构-活性关系。