Antimalarial activity of 4-(5-trifluoromethyl-1H-pyrazol-1-yl)-chloroquine analogues |
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Authors: | 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 |
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Institution: | Centro de Pesquisas René Rachou, Fiocruz e Departamento de Parasitologia-Universidade Federal de Minas Gerais (UFMG), Belo Horizonte, MG, Brazil. |
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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 (3)H]hypoxanthine in comparison to controls with no drugs. All but one of the eight (4,5-dihydropyrazol-1-yl) chloroquine 2 derivatives tested showed a significant activity in vitro, thus, are a promising new class of antimalarials. The three most active ones were also tested in vivo against Plasmodium berghei in mice. However, the (pyrazol-1-yl) chloroquine 3 derivatives were mostly inactive, suggesting that the aromatic functionality of the pyrazole ring was critical. |
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