Synthesis and in vitro evaluation of potential antichagasic hydroxymethyinitrofurazone (NFOH-121):: A new nitrofurazone prodrug

被引：77
作者：
Chung, MC
Güido, RVC
Martinelli, TF
Gonçalves, MF
Polli, MC
Botelho, KCA
Varanda, EA
Colli, W
Miranda, MTM
Ferreira, EI
机构：
[1] Univ Sao Paulo, Dept Farm, Fac Ciencias Farmaceut, BR-05389970 Sao Paulo, Brazil
[2] UNESP, Lapdesf Lab Pesquisa & Desenvolvimento Farm, Dept Farmacos & Med, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
[3] UNESP, Dept Ciencias Biol, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 22期
基金：
巴西圣保罗研究基金会;
关键词：
D O I：
10.1016/j.bmc.2003.07.004
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：
The synthesis of mutual prodrugs of nitrofurazone with primaquine, using specific and nonspecific spacer groups, has been previously attempted seeking selective antichagasic agents. The intermediate reaction product, hydroxymethylnitrofurazone (NFOH-121), was isolated and tested in LLC-MK2 culture cells infected with trypomastigotes forms of Trypanosoma cruzi showing higher trypanocidal activity than nitrofurazone and benznidazol in all stages. The mutagenicity tests showed that the prodrug was less toxic than the parent drug. Degradation assays were carried out in pH 1.2 and 7.4. (C) 2003 Elsevier Ltd. All rights reserved.
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页码：4779 / 4783
页数：5
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