Antiprotozoal Activity of (E)-Cinnamic N-Acylhydrazone Derivatives
AbstractA series of 14 (E)-cinnamic N-acylhydrazone derivatives, designed through molecular hybridization between the (E)-1-(benzo[d][1,3]dioxol-5-yl)-3-(4-bromophenyl)prop-2-en-1-one and (E)-3-hydroxy-N'-((2-hydroxynaphthalen-1-yl)methylene)-7-methoxy-2-naphthohydrazide, were tested for in vitro antiparasitic activity upon axenic amastigote forms of Leishmania donovani and bloodstream forms of Trypamosoma brucei rhodesiense. The derivative (2E)-3-(4-hydroxy-3-methoxy-5-nitrophenyl)-N'-[(1E)-phenylmethylene]acrylohydrazide showed moderate antileishmanial activity (IC50 = 6.27 µM) when compared to miltefosine, the reference drug (IC50 = 0.348 µM). However, the elected compound showed an excellent selectivity index; in one case it was not cytotoxic against mammalian L-6 cells. The most active antitrypanosomal compound, the derivative (E)-N'-(3,4-dihydroxybenzylidene)cinnamohydrazide (IC50 = 1.93 µM), was cytotoxic against mammalian L-6 cells. View Full-Text
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Carvalho, S.A.; Kaiser, M.; Brun, R.; Silva, E.F.; Fraga, C.A.M. Antiprotozoal Activity of (E)-Cinnamic N-Acylhydrazone Derivatives. Molecules 2014, 19, 20374-20381.
Carvalho SA, Kaiser M, Brun R, Silva EF, Fraga CAM. Antiprotozoal Activity of (E)-Cinnamic N-Acylhydrazone Derivatives. Molecules. 2014; 19(12):20374-20381.Chicago/Turabian Style
Carvalho, Samir A.; Kaiser, Marcel; Brun, Reto; Silva, Edson F.; Fraga, Carlos A.M. 2014. "Antiprotozoal Activity of (E)-Cinnamic N-Acylhydrazone Derivatives." Molecules 19, no. 12: 20374-20381.