Feit P W, Tvaermose Nielsen O B
J Med Chem. 1977 Dec;20(12):1687-91. doi: 10.1021/jm00222a033.
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.
制备了一系列与先前描述的3,4-二取代5-氨磺酰基苯甲酸利尿剂相对应的3,4-二取代5-酰氨基、5-烷基氨基和5-脲基苯甲酸，并在犬类中对其利尿特性进行了筛选。列表结果显示，几种3,4-二取代5-甲酰胺基和5-乙酰氨基苯甲酸具有相当大的利尿效力，这表明5-氨磺酰基或5-甲基磺酰基取代基对于3,4-二取代苯甲酸的高效利尿活性并非必需。4-苯甲酰基-3-苄氧基-5-甲酰胺基苯甲酸是本系列中最有效的化合物之一，其效力约为布美他尼的十分之一。剂量反应和利尿模式表明其具有高效能利尿活性，并提示其作用方式与布美他尼相似。
