Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents
Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents
复制标题
DOI：
10.1016/s0960-894x(00)00643-0
复制
发表时间：
2001-01-22
影响因子：
2.7
通讯作者：
O'Sullivan, MC
中科院分区：
文献类型：
--
作者：
Li, ZL;Fennie, MW;O'Sullivan, MC
合成了几种N-(3-苯丙基)取代亚精胺和精胺类化合物，发现它们是克氏锥虫色氨硫酮还原酶的有效竞争性抑制剂(描述了7个K-I值为lt；5M的化合物)。所研究的最有效的缓蚀剂是化合物12，其K-I值为0.151微米。所描述的化合物中有6种也是有效的杀锥虫剂，其IC50值
Several N-(3-phenylpropyl)-substituted spermidine and spermine derivatives were prepared and found to be potent competitive inhibitors of Trypanosoma cruzi trypanothione reductase (seven compounds with K-i values < 5 M are described). The most effective inhibitor studied was compound 12 with a K-i value of 0.151 muM. Six of the compounds described are also effective trypanocides with IC50 values