Synthesis and antimalarial activity of hydroxyethylpiperazine derivatives.
The antimalarial activity of hydroxyethylpiperazine derivatives, synthesized from the reaction of (2S,3S)Boc-phenylalanine epoxide with benzylpiperazines in good yields (76-96%), has been evaluated in vitro against the Plasmodium falciparum W2 clone (chloroquine resistant). The results show that some compounds have moderate activity against this parasite and none of the active compounds showed cytotoxicity at high concentration (100 microg/ml).
Cunico
Wilson
W
Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos, Farmanguinhos R. Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil. wjcunico@far.fiocruz.br
Gomes
Claudia R B
CR
Moreth
Marcele
M
Manhanini
Diogo P
DP
Figueiredo
Isabela H
IH
Penido
Carmen
C
Henriques
Maria G M O
MG
Varotti
Fernando P
FP
Krettli
Antoniana U
AU
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D002853:Chromatography, Liquid; D004353:Drug Evaluation, Preclinical; D004912:Erythrocytes / Q000469:parasitology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects*
D000962:Antimalarials; D010879:Piperazines