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

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.

Citation

Marius Trésor Dable, Konan Dominique Tano, Mahama Ouattara, Kigbafori Dieudonné Silue, Eby I Hervé Menan, William Yavo. Ex vivo efficacy of selective chalcone derivatives on reference strains and field isolates of Plasmodium falciparum. Pathogens and global health. 2019 Dec;113(8):359-363

Mesh Tags

Substances

PMID: 31910738

search → result