Novel 2-oxoquinoline-6-sulfonamides as thiazide-like diuretics

A series of novel N-aryl-7-chloro-4-methyl-2-oxo-1,2-dihydroquinoline-6-sulfonamides were obtained. The structure-activity relationship (SAR) approach was used to study their diuretic effect on rats. Diuretic activity was exhibited by all the test compounds, with 7-chloro-4-methyl-2-oxo-1,2-dihydroquinoline-6-sulfonanilide being most active. A SAR analysis revealed that the substituted (especially ortho-substituted in the benzene ring) arylamides diminish diuresis compared to the most active compound. For the most and least active compounds, their effects on the electrolyte excretion (Na+, K+, and Cl−) and creatinine level were also studied.