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Synthesis and Evaluation of New Antimalarial Phenylurenyl Chalcone Derivatives
journal contribution
posted on 2005-05-19, 00:00 authored by José N. Domínguez, Caritza León, Juan Rodrigues, Neira Gamboa de Domínguez, Jiri Gut, Philip J. RosenthalPhenylurenyl chalcone derivatives have been synthesized and tested as inhibitors of in vitro
development of a chloroquine-resistant strain of Plasmodium falciparum, activity of the cysteine
protease falcipain-2, in vitro globin hydrolysis, β-hematin formation, and murine Plasmodium
berghei malaria. The most active antimalarial compound was 1-[3‘-N-(N‘-phenylurenyl)phenyl]-3(3,4,5-trimethoxyphenyl)-2-propen-1-one 49, with an IC50 of 1.76 μM for inhibition of P.
falciparum development. Results suggest that chalcones exert their antimalarial activity via
multiple mechanisms.
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proteaseantimalarial compoundhematinstrainIC 50mechanismglobin hydrolysisNew Antimalarial Phenylurenyl Chalcone Derivatives Phenylurenyl chalcone derivativesEvaluationphenylurenylinhibitionPlasmodium falciparumfalcipainSynthesimurine Plasmodium berghei malariaantimalarial activityfalciparum developmentformation1.76 μ Mcysteineinhibitor
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