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.

(4-Methyl-2-oxo-1,2-dihydroquinoline-6-sulfonyl)acetanilides were obtained by either amidation of the respective acid with anilines or the reaction of N-aryl-2-chloroacetamide with 4-methyl-2-oxo-1,2-dihydroquinoline-6-sulfinic acid. Screening of the synthesized compounds revealed their hemostatic activity in vitro.