Aromatic guanyl hydrazones: Synthesis, structural studies and in vitro activity against Trypanosoma cruzi

被引：43
|
作者：
Messeder, JC
Tinoco, LW
FigueroaVillar, JD
Souza, EM
Rita, RS
deCastro, SL
机构：
[1] INST MIL ENGN,DEPT QUIM,BR-22290270 RIO JANEIRO,BRAZIL
[2] INST OSWALDO CRUZ,DEPT ULTRAESTRUTURA & BIOL CELULAR,BR-21045900 RIO JANEIRO,BRAZIL
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 24期
关键词：
D O I：
10.1016/0960-894X(95)00541-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 22 aromatic guanyl hydrazones, prepared by condensation of several aldehydes with aminoguanidine hydrochloride, were fully characterized by NMR techniques and tested in vitro against the trypomastigote form of Trypanosoma cruzi, the causative agent of Chagas disease. Most of the compounds, especially those without hydrogen bonding groups and possessing ortho-substitution, were significantly more active than crystal violet (ID50 536 mu M). The most active compound has an ID50 value of 17 mu M (25 times more potent than gentian violet).
引用
收藏
页码：3079 / 3084
页数：6
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