ChemInform Abstract: Second Generation of 2H-Benzimidazole 1,3-Dioxide Derivatives as anti-Trypanosomatid Agents: Synthesis, Biological Evaluation, and Mode of Action Studies

Autor:	Agustina Chidichimo, Hugo Cerecetto, Alicia Merlino, Mercedes González, Paola Hernández, Mariana Boiani, Lucía Boiani, Juan José Cazzulo
Rok vydání:	2010
Předmět:	Benzimidazole biology General Medicine biology.organism_classification Leishmania braziliensis Glycosome chemistry.chemical_compound chemistry Mechanism of action Biochemistry Benznidazole parasitic diseases medicine medicine.symptom Trypanosoma cruzi Mode of action Amastigote medicine.drug
Zdroj:	ChemInform. 41
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.201009128
Popis:	Exploring the influence of different substitution patterns of 2H-benzimidazole 1,3-dioxide derivatives (BzNO) we prepared fifteen new derivatives. Initially the BzNO were tested against Trypanosoma cruzi Tulahuen 2 strain epimastigote form rendering very potent anti-T. cruzi agents. Moreover, the BzNO were able to inhibit the growth of virulent and resistant to Benznidazole strains (CL Brener clone, Colombiana, and Y strains) and to Leishmania braziliensis. Interestingly, BzNO exhibited very high selectivity index and particularly the spiro-BzNO 13 provokes an important diminution of amastigotes in Vero cells. Besides, it was found a diminution of acetate and glycine as excreted metabolites but without increase of parasite glucose uptake indicating that the glycosome is probably not involucrate in the 2H-benzimidazole 1,3-dioxides mechanism of action.
Databáze:	OpenAIRE
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