[Structure-activity relationships in the diuretic xipamide (4-chloro-5-sulfamoyl-2', 6' -salicyloxylidide)].


The synthesis of various derivatives of 4-chlorosalicylic acid substituted in position 5 is described. The evaluation of their diuretic potency on the rat showed 4-chloro-5-sulfamoyl-2,6-salicyloxylidide (BE 1293, xipamide, Aquaphor) as the most effective one. The normal urinary volume is increased tenfold by a oral dose of 100 mg/kg body weight. All… (More)