Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 80, Issue 2, Pages 340-347Publisher
WILEY
DOI: 10.1111/j.1747-0285.2012.01383.x
Keywords
antimalarial activity; Chalcone synthesis; in vitro; Plasmodium falciparum
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Twenty-seven novel chalcone derivatives were synthesized using Claisen-Schmidt condensation and their antimalarial activity against asexual blood stages of Plasmodium falciparum was determined. Antiplasmodial IC50 (half-maximal inhibitory concentration) activity of a compound against malaria parasites in vitro provides a good first screen for identifying the antimalarial potential of the compound. The most active compound was 1-(4-benzimidazol-1-yl-phenyl)-3-(2, 4-dimethoxy-phenyl)-propen-1-one with IC50 of 1.1 mu g/mL, while that of the natural phytochemical, licochalcone A is 1.43 mu g/mL. The presence of methoxy groups at position 2 and 4 in chalcone derivatives appeared to be favorable for antimalarial activity as compared to other methoxy-substituted chalcones. Furthermore, 3, 4, 5-trimethoxy groups on chalcone derivative probably cause steric hindrance in binding to the active site of cysteine protease enzyme, explaining the relative lower inhibitory activity.
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