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鉴于黄嘌呤类化合物具有咖啡因、茶碱相似的强心利尿作用以及合成的嘧啶类化合物3-烯丙基-6-氨基-1-乙基尿嘧啶和-6-氨基-1,3-二乙基-5-异丙基尿嘧啶具有利尿作用。作者乃合成Ⅰ、Ⅱ和Ⅲ类共79个化合物,并研究其结构与疗效的关系。其中 I_(a～e)和Ⅱ的利尿作用与咖啡因相等或更强些,而 I_(b,c)的强心作用比咖啡因强。其中以 I_(e,f)的中枢神经兴奋作用为最强。实验结果表明:Ⅰ和Ⅱ的7-位氮原子是具有类似咖啡因作用所必需的。
In view of xanthine compounds with caffeine, theophylline similar cardiac diuretic effect and the synthesis of pyrimidine compounds 3-allyl-6-amino-1-ethyluracil and 6-amino-1,3-bis Ethyl-5-isopropyl uracil has diuretic effect. The authors synthesized a total of 79 compounds of type I, II and III and studied the relationship between their structure and efficacy. The diuretic effects of I_ (a ~ e) and Ⅱ were equal to or stronger than those of caffeine, whereas the I_ (b, c) had stronger cardiac effects than caffeine. Among them, I_ (e, f) of the central nervous excitement is strongest. The experimental results show that the nitrogen atoms at the 7-position of Ⅰ and Ⅱ are necessary for caffeine-like effect.