Synthesis and in vitro antiprotozoal evaluation of substituted phenalenone analogues.
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.
Rosquete
Laura I
LI
Instituto Universitario de Bio-Orgánica 'Antonio González', Universidad de La Laguna, La Laguna, Tenerife, Canary Islands, Spain.
Cabrera-Serra
M Gabriela
MG
Piñero
José E
JE
Martín-Rodríguez
Patricia
P
Fernández-Pérez
Leandro
L
Luis
Javier G
JG
McNaughton-Smith
Grant
G
Abad-Grillo
Teresa
T
D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D045744:Cell Line, Tumor; D006801:Humans; D007896:Leishmaniasis / Q000188:drug therapy; D010419:Pentamidine / Q000627:therapeutic use; D043803:Phenalenes / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects; D014352:Trypanosomiasis / Q000188:drug therapy
D000981:Antiprotozoal Agents; D043803:Phenalenes; C038036:phenalen-1-one; D010419:Pentamidine