TY - JOUR
T1 - Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds
AU - Olmo, Esther Del
AU - Barboza, Bianca
AU - Chiaradia, Louise D.
AU - Moreno, Alicia
AU - Carrero-Lérida, Juana
AU - González-Pacanowska, Dolores
AU - Muñoz, Victoria
AU - López-Pérez, José L.
AU - Giménez, Alberto
AU - Benito, Agustín
AU - Martínez, Antonio R.
AU - Ruiz-Pérez, Luis M.
AU - San Feliciano, Arturo
PY - 2011/11
Y1 - 2011/11
N2 - 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.
AB - 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.
KW - Imidazoisoindoles
KW - In vitro assays
KW - In vivo assays
KW - Mouse model
KW - Plasmodium berghei
KW - Plasmodium falciparum
KW - Structure-activity relationship
KW - Synthesis
UR - http://www.scopus.com/inward/record.url?scp=80054907453&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2011.08.043
DO - 10.1016/j.ejmech.2011.08.043
M3 - Artículo
C2 - 21940072
AN - SCOPUS:80054907453
VL - 46
SP - 5379
EP - 5386
JO - CHIM.THER.
JF - CHIM.THER.
SN - 0223-5234
IS - 11
ER -