Marr J J, Berens R L, Cohn N K, Nelson D J, Klein R S
Antimicrob Agents Chemother. 1984 Feb;25(2):292-5. doi: 10.1128/AAC.25.2.292.
Previous investigations have suggested that inosine analogs would be good models for the development of chemotherapeutic agents active against pathogenic hemoflagellates. We have systematically modified the five-membered heterocyclic ring of six inosine analogs and tested them for their antiprotozoal activities and toxicity to a mammalian cell line. All six analogs were very active against the three protozoan pathogens Leishmania donovani, Trypanosoma cruzi, and Trypanosoma gambiense. Two of the six, 9-deazainosine and allopurinol ribonucleoside, had very little toxicity for mouse L cells and offer promise as potential chemotherapeutic agents.
先前的研究表明,肌苷类似物将是开发对致病性血鞭毛虫有效的化疗药物的良好模型。我们系统地修饰了六种肌苷类似物的五元杂环,并测试了它们的抗原生动物活性和对哺乳动物细胞系的毒性。所有六种类似物对三种原生动物病原体杜氏利什曼原虫、克氏锥虫和冈比亚锥虫都非常有效。六种中的两种,即9-脱氮肌苷和别嘌呤醇核糖核苷,对小鼠L细胞的毒性很小,有望成为潜在的化疗药物。