Ex vivo efficacy of selective chalcone derivatives on reference strains and field isolates of Plasmodium falciparum

选择性查尔酮衍生物对恶性疟原虫参考株和野生分离株的体外疗效

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作者:Marius Trésor Dable, Konan Dominique Tano, Mahama Ouattara, Kigbafori Dieudonné Silue, Eby I Hervé Menan, William Yavo

Abstract

The extension of Plasmodium falciparum resistance to existing antimalarial drugs is worrying. Faced with this problem, the search for new and effective molecules is necessary. In this context, six chalcone derivatives (B1, B11, B14, B17, SCA02 and SCA03) were tested on field isolates and then reference strains to evaluate their antiplasmodial activity by using the Rieckmann semi-microtest, recommended by WHO, for in vitro and ex vivo activity tests. Compounds B14 and B17 exhibited promising antiplasmodial activities (IC50s: 14.41-16.40 μM) regardless of the type of isolate. Compounds B1, B11, SCA02 and SCA03 showed a moderate inhibition of field isolates (IC50S: 25.63-48.29 μM) and very good activity against reference strains (IC50s: 3.82-10.03 μM). Therefore, more structural modulations should improve their efficiency and make these molecules very good candidates for future effective antimalarial drugs.

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