Title of article :
Studies on quinones. Part 39: Synthesis and leishmanicidal activity of acylchloroquinones and hydroquinones Original Research Article
Author/Authors :
Jaime A. Valderrama، نويسنده , , Carlos Zamorano، نويسنده , , M. Florencia Gonz?lez، نويسنده , , Eric Prina، نويسنده , , Alain Fournet، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
Abstract :
Acylhydroquinone-based compounds are attractive targets for the design of new leishmanicidal drugs. We have previously described sesquiterpene quinones and hydroquinones series, which exhibit different degree of potency against Leishmania amazonensis. The present study details the preparation of acylchloroquinones and hydroquinones possessing lipophilic substituents and examines their in vitro activity against intracellular L. amazonensis amastigotes. The quinone or hydroquinone nucleus is essential for the activity of the members of the series. The lipophilicity of the cycloaliphatic systems in these members seems to attenuate the cytotoxical effect and increases the selectivity of those compounds containing the norbornene system.
Keywords :
Enolization , Diels–Alder reaction , Quinones , Lipophilicity , leishmanicidal activity
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry