New potent imidazoisoquinolinone derivatives as anti-Trypanosoma cruzi agents: Biological evaluation and structure-activity relationships

被引：47
|
作者：
Bollini, Mariela [1 ]
Jose Casal, Juan [1 ]
Alvarez, Diego E. [1 ]
Boiani, Lucia [2 ,3 ]
Gonzalez, Mercedes [2 ,3 ]
Cerecetto, Hugo [2 ,3 ]
Maria Bruno, Ana [1 ]
机构：
[1] Univ Buenos Aires, Fac Farm & Bioquim, Dept Quim Organ, RA-1113 Buenos Aires, DF, Argentina
[2] Univ Republica, Dept Quim Organ, Fac Ciencias, Montevideo, Uruguay
[3] Univ Republica, Fac Quim, Montevideo, Uruguay
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 04期
关键词：
Imidazoisoquinolinones; QSAR; anti-Trypanosoma cruzi agents; LEISHMANIA; METABOLISM; ACIDS;
D O I：
10.1016/j.bmc.2009.01.011
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of novel benzoimidazo andN-aryl-5-oxo-imidazo[1,2-b] isoquinoline-10-carbothioamides was developed. All the compounds were evaluated for their in vitro action against the epimastigote form of Trypanosoma cruzi. Four of them showed higher activity than Nifurtimox. Their unspecific cytotoxicity was evaluated using HeLa and L6 cells, being non-toxic at concentrations at least 15 and 200 times higher than that of T. cruzi IC50. To gain insight into the mechanism of action, their DNA binding properties and reactivity with glutathione were studied, and QSAR study was performed. (c) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1437 / 1444
页数：8
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