42086-72-6Relevant articles and documents
Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds
Olmo, Esther Del,Barboza, Bianca,Chiaradia, Louise D.,Moreno, Alicia,Carrero-Lérida, Juana,González-Pacanowska, Dolores,Mu?oz, Victoria,López-Pérez, José L.,Giménez, Alberto,Benito, Agustín,Martínez, Antonio R.,Ruiz-Pérez, Luis M.,San Feliciano, Arturo
experimental part, p. 5379 - 5386 (2011/12/14)
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 IC50 values as low as 60 nM and a certain efficacy in vivo by reducing parasitemia in Plasmodium berghei mouse models.
Vasorelaxant activity of phthalazinones and related compounds
Olmo, Esther del,Barboza, Bianca,Ybarra, Ma Ines,Lopez-Perez, Jose Luis,Carron, Rosalia,Sevilla, Ma Angeles,Boselli, Cinthia,Feliciano, Arturo San
, p. 2786 - 2790 (2007/10/03)
Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10-5 M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC50 = 0.43 μM) the affinities for α1A, α1B and α1D adrenergic sub-receptors were determined.
