Monge A, Martinez-Merino V, Sanmartin C, Fernandez F J, Ochoa M C, Bellver C, Artigas P
Departamento de Química Orgánica y Farmaceútica, Universidad de Navarra, Pamplona, Spain.
Arzneimittelforschung. 1990 Nov;40(11):1230-3.
The synthesis of a series of 12 compounds referring to 4-anilino-2-methylthiopyrido [2,3-d]pyrimidines (1-12), and the results of a study of their diuretic, saliuretic and antihypertensive activities are reported. Most of this compounds showed significant diuretic activity at the dosage of 3-24 mg/kg. The 4-Anilino-2-methylthiopirido[2,3-d]pyrimidine 1 remained active to a dosage of 1 mg/kg. The diuretic activity of these compounds implied an increase in the Na+ excretion. Some of the most active diuretics have been studied for antihypertensive effect.
报道了一系列12种涉及4-苯胺基-2-甲基硫代吡啶并[2,3-d]嘧啶(1-12)的化合物的合成,以及它们的利尿、利盐和降压活性的研究结果。这些化合物中的大多数在3-24mg/kg的剂量下表现出显著的利尿活性。4-苯胺基-2-甲基硫代吡啶并[2,3-d]嘧啶1在1mg/kg的剂量下仍保持活性。这些化合物的利尿活性意味着Na+排泄增加。对一些活性最强的利尿剂进行了降压作用研究。