Lee C M, Plattner J J, Ours C W, Horrom B W, Smital J R, Pernet A G, Bunnell P R, El Masry S E, Dodge P W
J Med Chem. 1984 Dec;27(12):1579-87. doi: 10.1021/jm00378a010.
A series of Mannich bases and aminomethyl derivatives of ethyl [2,3-dichloro-4-(4-hydroxybenzoyl)phenoxy]acetate were synthesized and tested for saluretic and diuretic activities. The effects of nitrogen and aromatic nuclear substitution, reorientation of the aminomethyl group relative to that of the phenolic hydroxyl group, and replacement of either the phenolic hydroxyl or the aminomethyl group by other functional groups are described. Ethyl [2,3-dichloro-4-[3-(aminomethyl)-4-hydroxybenzoyl]phenoxy]acetate (27) was found to be a very potent, high-ceiling diuretic.
合成了一系列[2,3-二氯-4-(4-羟基苯甲酰基)苯氧基]乙酸乙酯的曼尼希碱和氨甲基衍生物，并对其利尿和促尿钠排泄活性进行了测试。描述了氮和芳环取代、氨甲基相对于酚羟基的重新定向以及酚羟基或氨甲基被其他官能团取代的影响。发现[2,3-二氯-4-[3-(氨甲基)-4-羟基苯甲酰基]苯氧基]乙酸乙酯(27)是一种非常有效的高效能利尿剂。
