Design, Synthesis, and Biological Evaluation of New Growth Inhibitors of <i>Trypanosoma cruzi</i> (Epimastigotes)
作者:Andrea J. Schvartzapel、Li Zhong、Roberto Docampo、Juan B. Rodriguez、Eduardo G. Gros
DOI:10.1021/jm9607616
日期:1997.7.1
search for new chemotherapeutic agents against Chagas' disease, several drugs structurally related to the insect growth regulator Fenoxycarb and the naturally occurring juvenile hormone of insects were designed, synthesized, and evaluated as antiproliferative agents against the parasite responsible of this disease. Isoprenoid derivatives (compounds 33, 34, 36, and 37) were potent growth inhibitors of Trypanosoma
作为我们旨在寻找新的针对查加斯病的化学治疗剂的项目的继续,设计,合成并评估了几种与昆虫生长调节剂苯氧威和天然存在的昆虫幼体激素有关的药物,作为抗寄生虫的抗增殖剂对这种疾病负责。类异戊二烯衍生物(化合物33、34、36和37)是克鲁斯锥虫锥鞭毛虫的有效生长抑制剂。另外,考虑到对化合物30观察到的高活性和相关化合物的抑制作用,在这些抑制剂的极性极端处结合的烯丙基醚部分被证明是设计新药的有希望的基团。