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

2019; Taylor & Francis; Volume: 113; Issue: 8 Linguagem: Inglês

10.1080/20477724.2019.1710065

2047-7732

Marius Trésor Dable, Konan Dominique Tano, Mahama Ouattara, Kigbafori D. Silué, Eby Ignace Hervé Menan, William Yavo,

Traditional and Medicinal Uses of Annonaceae

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.