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Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.

Abstract：

:The ruthenium complex, trans-[Ru(Bz)(NH 3) 4SO 2](CF 3SO 3) 2 1, Bz = benznidazole ( N-benzyl-2-(2-nitro-1 H-imidazol-1-yl)acetamide), is more hydrosoluble and more active (IC 50try/1 h = 79 +/- 3 microM) than free benznidazole 2 (IC 50try/1 h > 1 mM). 1 also exhibits low acute toxicity in vitro (IC 50macrophages > 1 mM) and in vivo (400 micromol/kg < LD 50 < 600 micromol/kg) and the formation of hydroxylamine is more favorable in 1 than in 2 by 9.6 kcal/mol. In murine acute models of Chagas' disease, 1 was more active than 2 even when only one dose was administrated. Moreover, 1 at a thousand-fold smaller concentration than the considered optimal dose for 2 (385 micromol/kg/day = 100 mg/kg/day), proved to be sufficient to protect all infected mice, eliminating the amastigotes in their hearts and skeletal muscles as observed in H&E micrographics.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Nogueira Silva JJ,Pavanelli WR,Gutierrez FR,Alves Lima FC,Ferreira da Silva AB,Santana Silva J,Wagner Franco D

doi

10.1021/jm701306r

subject

Has Abstract

pub_date

2008-07-24 00:00:00

pages

4104-14

issue

14

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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