- Structure activity relationship for derivatives of xipamide (4 chloro 5 sulfamoyl 2',6' salicyloxylidide)
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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. The normal urinary volume is increased 10 fold by an oral dose of 100 mg/kg body weight. All changes in the molecular structure of xipamide, even acetylation, the introduction of a second sulfamoyl group or the exchange of the sulfonic group for the carbonyl group lead to a decrease in activity.
- Liebenow,Leuschner
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p. 240 - 244
(2007/10/09)
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