Bioorganic & Medicinal Chemistry 2010-06-15

Synthesis and in vitro antiprotozoal evaluation of substituted phenalenone analogues.

Laura I Rosquete, M Gabriela Cabrera-Serra, José E Piñero, Patricia Martín-Rodríguez, Leandro Fernández-Pérez, Javier G Luis, Grant McNaughton-Smith, Teresa Abad-Grillo

Index: Bioorg. Med. Chem. 18(12) , 4530-4, (2010)

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Abstract

A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiparasitic activities against the most clinically relevant forms of trypanosomiasis and leishmaniasis. Several compounds exhibited leishmanicidal effects at levels comparable or better than the reference drug pentamidine, while the parent phenalenone was shown to have a level of activity against Trypanosoma cruzi comparable to the marketed drug benznidazole.Copyright 2010 Elsevier Ltd. All rights reserved.