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Synthesis and in vitro antiprotozoal evaluation of substituted phenalenone analogues |
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| Authors: | 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 |
| Institution: | 1. Instituto Universitario de Bio-Orgánica ‘Antonio González’, Universidad de La Laguna, Avda. Fco., Sánchez 2, 38206 La Laguna, Tenerife, Canary Islands, Spain;2. Instituto Universitario de Enfermedades Tropicales y Salud Pública de Las Islas Canarias, Laboratorio de Quimioterapias de Protozoos, Universidad de La Laguna, Avda. Francisco Sánchez s/n, 38206 La Laguna, Tenerife, Canary Islands, Spain;3. Department of Clinical Sciences, Molecular and Translational Endocrinology Group, University of Las Palmas de GC—Cancer Research Institute of the Canary Islands (ICIC), Spain;4. CEAMED, SA, Spain |
| 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. |
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