Estudo visando a síntese enantiosseletiva da dictiolomida e da 6-metoxidictiolomida : síntese e avaliação biológica de derivados quinolinônicos / TOWARDS OF ENANTIOSELECTIVE SYNTHESIS OF DICTYOLOMIDE A AND 6-METHOXIDICTYOLOMIDE: SYNTHESIS AND BIOLOGICAL EVALUATION OF QUINOLINONICS DERIVATIVES

AUTOR(ES)
DATA DE PUBLICAÇÃO

2007

RESUMO

Dictyolomide A (13) and 6-methoxydictyolomide (15) were isolated from plants of the Dictyoloma genus, therefore their structures were not yet completely elucidated due to the C-3 stereocenter. These compounds showed an interesting biological activity against different forms of Leishmania sp., protozoa responsible for leishmaniose. In this work is described the study towards the enantioselective synthesis of 13 e 15 in order to confirm their stereochemistry and biological activity. The employed methodologies were based on literature described by NAKATSU et al. (1990) and EDMONT et al. (2000). In parallel, a small library of quinoline derivatives was prepared. This library and synthetic intermediates were evaluated against different forms of Leishmania and APTR enzyme from L. tarentolae, to confirm the leishmanicidal activity of the quinolinone systems. Furthermore, a wide biological evaluation was performed with these compounds employing bioassays to measure activity against snake venoms, PNP enzyme from Schistosoma mansoni, and phytotoxic activity to obtain information for studies of structure activity relationship.

ASSUNTO(S)

avaliação biológica química orgânica derivados quinolinônicos 6-metoxidictiolomida dictiolomida síntese enantiosseletiva quimica

ACESSO AO ARTIGO

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