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Synthesis and in vitro trypanocide activity of several polycyclic drimane-quinone derivatives.

Bioorganic & medicinal chemistry (2003-05-22)
Mauricio A Cuellar, Cristian Salas, Manuel J Cortés, Antonio Morello, Juan Diego Maya, Marcelo D Preite
RESUMEN

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.

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Tebbe reagent solution, 0.5 M in toluene