Abstract
The Diels-Alder reaction between two polygodial-derived dienes and simple quinones to yield substituted naphtho- and anthraquinones, is described. The in vitro trypanocide activity for the series was determined. Two of the new compounds showed an activity ten and two times higher, respectively, than nifurtimox and benznidazole, the medicines of choice for the treatment of the acute Chagas' disease.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Inhibitory Concentration 50
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Nifurtimox / pharmacology
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Nitroimidazoles / pharmacology
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Polycyclic Compounds / chemical synthesis
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Polycyclic Compounds / pharmacology
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Polycyclic Sesquiterpenes
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Quinones / chemical synthesis*
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Quinones / chemistry
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Quinones / pharmacology*
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Sesquiterpenes / chemical synthesis*
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Sesquiterpenes / chemistry
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Sesquiterpenes / pharmacology*
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Trypanocidal Agents / chemical synthesis*
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Trypanocidal Agents / chemistry
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Trypanocidal Agents / pharmacology*
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Trypanosoma cruzi / drug effects
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Trypanosoma cruzi / growth & development
Substances
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Nitroimidazoles
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Polycyclic Compounds
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Polycyclic Sesquiterpenes
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Quinones
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Sesquiterpenes
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Trypanocidal Agents
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drimane
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Nifurtimox
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benzonidazole