Novel Derivatives of Kaurenoic Acid

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...

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Bibliographic Details
Published in:Journal of the Brazilian Chemical Society 2002, Vol.13 (2), p.151-157
Main Authors: Vieira, Henriete S., Takahashi, Jacqueline A., Oliveira, Alaíde B. de, Chiari, Egler, Boaventura, Maria Amélia D.
Format: Article
Language:English
Subjects:
CHEMISTRY, MULTIDISCIPLINARY
kauranic oximes
kaurenic hydrochloride salts
kaurenoic acid
trypanocidal activity
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Summary: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.
ISSN:0103-5053
1678-4790
DOI:10.1590/S0103-50532002000200004