Ress R W, Chai S Y, Winkley M W, Russell R B
J Med Chem. 1976 May;19(5):723-5. doi: 10.1021/jm00227a029.
Thirteen new analogs of 2,4-diamino-5(p-chlorophenyl)-6-ethylpyrimidine (Daraprim, pyrimethamine) in which the alph position of the 6-ethyl substituent was modified were prepared. The respective oxygens analogs (ketals, ketone, alcohol), the dimethyl hydrazone, and the nitrone displayed activities in the range of 1/4 to 1/16 that of pyrimethamine toward Plasmodium berghei in mice. The therapeutic ratios of some of these compounds may be slightly better than that of pyrimethamine.
制备了13种2,4-二氨基-5-(对氯苯基)-6-乙基嘧啶（达拉匹林，乙胺嘧啶）的新类似物，其中6-乙基取代基的α位被修饰。相应的氧类似物（缩酮、酮、醇）、二甲基腙和硝酮对小鼠体内的伯氏疟原虫显示出的活性为乙胺嘧啶活性的1/4至1/16。其中一些化合物的治疗指数可能略优于乙胺嘧啶。
