Firth W J, Messa A, Reid R, Wang R C, Watkins C L, Yielding L W
J Med Chem. 1984 Jul;27(7):865-70. doi: 10.1021/jm00373a010.
Twenty-four acridine derivatives were screened for trypanocidal activity in Trypanosoma brucei in order to determine which structural features of the acridine molecule confer maximal antiparasitic activity. The synthesis of several new azidoacridine derivatives are also reported as well as an assessment of their value as possible photoaffinity probes for the study of acridine trypanocidal action. The most effective and selective acridine trypanocides, with and without irradiation, were the 3-amino-10-methylacridinium salt derivatives. With brief irradiation, one azidoacridine, 3-amino-6-azido-10-methylacridinium chloride, showed considerable trypanocidal activity at very limiting drug concentrations (10(-7)M) and warrants consideration as a possible photoaffinity probe.
筛选了24种吖啶衍生物对布氏锥虫的杀锥虫活性，以确定吖啶分子的哪些结构特征赋予最大的抗寄生虫活性。还报道了几种新的叠氮吖啶衍生物的合成，以及对它们作为研究吖啶杀锥虫作用的可能光亲和探针的价值评估。最有效和选择性的吖啶杀锥虫剂，无论有无照射，都是3-氨基-10-甲基吖啶鎓盐衍生物。经过短暂照射，一种叠氮吖啶，即3-氨基-6-叠氮-10-甲基吖啶鎓氯化物，在非常低的药物浓度（10(-7)M）下显示出相当大的杀锥虫活性，值得考虑作为一种可能的光亲和探针。
