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vol.13 issue2Baseline Studies on Water and Sediments in the Copper Mining Region of Salobo-3A, Carajas: Amazon, BrazilSynthesis of Cyclohexyl 6-O-Trityl-alpha-D-Threo-Hexopyranosid-4-ulo-(2,3:3',4')-2-Pyrazoline author indexsubject indexarticles search
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Journal of the Brazilian Chemical Society

Print version ISSN 0103-5053On-line version ISSN 1678-4790


VIEIRA, Henriete S. et al. Novel Derivatives of Kaurenoic AcidPreparation and Evaluation of their Trypanocidal Activity. J. Braz. Chem. Soc. [online]. 2002, vol.13, n.2, pp.151-157. ISSN 1678-4790.

Kaurenoic acid, a kauranic diterpenoid, presents in vitro activity against trypomastigote forms of Trypanosoma cruzi, showing, however, lytic activity on blood erythrocytes, as a side effect. The syntheses of twelve new derivatives of kaurenoic acid, four amides, four amines (and three hydroclorides) and four oximes, was carried out aiming at the improvement of the therapeutic activity and without the side effect. Among the derivatives prepared, one compound showed enhanced trypanocidal activity in vitro towards Trypanosoma cruzi trypomastigote erythrocytic forms, when compared to kaurenoic acid, but continued to show discrete lytic activity on erythrocytes; another compound showed a level of activity similar to that of kaurenoic acid, but without lysis.

Keywords : kaurenoic acid; kaurenic hydrochloride salts; kauranic oximes; trypanocidal activity.

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