Gatta F, Gradoni L, Lupardini E, Gramiccia M, Orsini S
Laboratorio di Chimica del Farmaco, Instituto Superiore di Sanità, Roma.
Farmaco. 1991 Jan;46(1):75-84.
Several new derivatives of 4-amino-, 4,6-diamino- and 4-hydrazino-[3,4-d]pyrimidine dihydroxyalkyl substituted in the 1 or 2 positions, or dihydroxyalkoxy substituted in the 3 position have been synthesized. Some of these compounds were evaluated for their activity against Leishmania infantum in mice. The highest degree of antileishmanial activity was displayed by the 4-amino-1-(dihydroxyalkyl) derivatives which yielded parasite inhibition values nearly comparable with that of glucantime in a standard 5-day test.
已经合成了几种1或2位被二羟基烷基取代、或3位被二羟基烷氧基取代的4-氨基-、4,6-二氨基-和4-肼基-[3,4-d]嘧啶的新衍生物。对其中一些化合物在小鼠体内抗婴儿利什曼原虫的活性进行了评估。4-氨基-1-(二羟基烷基)衍生物表现出最高程度的抗利什曼原虫活性，在标准的5天试验中，其产生的寄生虫抑制值几乎与葡糖胺锑相当。
