Feit Pw, Tvaermose Nielsen Ob
Dec 1, 1977
Citations
0
Influential Citations
2
Citations
Quality indicators
Journal
Journal of Medicinal Chemistry
Abstract
: A number of 3,4-disubstituted 5-acylamino-, 5-alkylamino-, and 5-ureidobenzoic acids corresponding to previously described 3,4-disubstituted 5-sulfamoylbenzoic acid diuretics were prepared and screened for their diuretic properties in dogs. The tabulated results reveal that several 3,4-disubstituted 5-formamido and 5-acetamidobenzoic acids possess considerable diuretic potency demonstrating that a 5-sulfamoyl or 5-methylsulfonyl substituent is not a necessity for potent diuretic activity of 3,4-disubstituted benzoic acids. 4-Benzoyl-3-benzyloxy-5-formamidobenzoic acid, one of the mo-t potent compounds of the present series, is approximately one-tenth as potent as bumetanide. The dose response and diuretic pattern indicate high-ceiling diuretic activity and suggest a mode of action similar to that of bumetanide.