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2030-01-01
Sustainable Development Goals
03 Saúde e Bem-EstarCollections
- IOC - Artigos de Periódicos [12969]
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SYNTHESIS AND BIOLOGICAL EVALUATION OF N-ALKYL NAPHTHOIMIDAZOLES DERIVED FROM β-LAPACHONE AGAINST TRYPANOSOMA CRUZI BLOODSTREAM TRYPOMASTIGOTES
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Abstract
The QSAR study of 34 2-aryl-naphthoimidazoles screened so far revealed that σi is the most important factor
for their lytic activity on the bloodstream trypomastigote forms of T. cruzi, the etiologic agent of
Chagas disease. Based on this result, 16 new N-alkyl-naphthoimidazoles derived from 6,6-dimethyl-
3,4,5,6-tetrahydrobenzoij7,8]chromeneij5,6-d]imidazole (the product of the reaction of β-lapachone with
paraformaldehyde) by its reaction with halo-alkanes were prepared and evaluated against the parasite and
peritoneal macrophages. The N1-n-hexyl and N3-n-hexyl naphthoimidazoles were 2.2 and 3.2 times more
active than the standard drug benznidazole with selectivity indices of 2.7 and 13.4, respectively.
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