Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds

Esther Del Olmo, Bianca Barboza, Louise D. Chiaradia, Alicia Moreno, Juana Carrero-Lérida, Dolores González-Pacanowska, Victoria Muñoz, José L. López-Pérez, Alberto Giménez, Agustín Benito, Antonio R. Martínez, Luis M. Ruiz-Pérez, Arturo San Feliciano

Producción científica: Contribución a una revistaArtículorevisión exhaustiva

20 Citas (Scopus)

Resumen

The synthesis of several series of imidazo[2,1-a]isoindol-5-ol derivatives and the results of their evaluation against Plasmodium falciparum are presented and discussed. The effects of electron-withdrawing or-donating substituents on different parts of the molecule, as well as those produced by the incorporation of an additional fused ring, were analyzed. Several compounds showed significant antimalarial activity in vitro with IC 50 values as low as 60 nM and a certain efficacy in vivo by reducing parasitemia in Plasmodium berghei mouse models.

Idioma originalInglés
Páginas (desde-hasta)5379-5386
Número de páginas8
PublicaciónEuropean Journal of Medicinal Chemistry
Volumen46
N.º11
DOI
EstadoPublicada - nov. 2011

Nota bibliográfica

Funding Information:
Authors thank Dr. Carmen Cuevas (PharmaMar S.A. Madrid, Spain) for cytotoxicity assays and to Bioinformatic & Molecular Design Research Center (BMDRC, Yonsey University, Seoul, Korea) for complimentary access to preADMET database. BB and LDC thank the respective fellowships from ALFA (ALR/B73011/94.04-6.0275.9) and ALBAN (E07D401988BR) EC Programs. Financial support from FIS-PI-060782 , FIS-PI-052026 , SAF2010-20059 , the “Plan Andaluz de Investigación (BIO199 )” and ISCIII-RICET ( RD06/0021: 0000 , 0018, 0022 ) is also acknowledged.

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