Antimalarial activity of 4-(5-trifluoromethyl-1H-pyrazol-1-yl)-chloroquine analogues

W Cunico, CA Cechinel, HG Bonacorso…

Index: Cunico, Wilson; Cechinel, Cleber A.; Bonacorso, Helio G.; Martins, Marcos A. P.; Zanatta, Nilo; De Souza, Marcus V.N.; Freitas, Isabela O.; Soares, Rodrigo P. P.; Krettli, Antoniana U. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 3 p. 649 - 653

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Citation Number: 99

Abstract

The antimalarial activity of chloroquine-pyrazole analogues, synthesized from the reaction of 1, 1, 1-trifluoro-4-methoxy-3-alken-2-ones with 4-hydrazino-7-chloroquinoline, has been evaluated in vitro against a chloroquine resistant Plasmodium falciparum clone. Parasite growth in the presence of the test drugs was measured by incorporation of [3H] hypoxanthine in comparison to controls with no drugs. All but one of the eight (4, 5- ...