Synthesis and Heme Polymerization Inhibitory Activity (HPIA) Assay of Chalcone, Flavone and Flavanone Derivatives

Chalcone, flavone, and flavanone had been synthesized as candidate of the antimalarial compounds. The chalcone 1was synthesised from 2,4-dihydroxyacetophenone and 4-metoxybenzaldehyde as starting materials using base catalyst KOH via Claisen-Schmidt Condensation. The synthesis flavone 2was carried out by cyclization of chalcone 1using I 2 in DMSO, while the flavanone 3was produced by cyclization of chalcone 1using NaOAc as a base catalyst. An in vitro antimalarial activity of the compound 1, 2and 3have been evaluated with the chloroquine diphosphate as a positive control in various concentration, and this assay was carried out according to the Basilico method. The IC 50 value of compound 1, 2, 3and a positive control were 0.25; 0.62; 1.33 and 0.35 mM, respectively. The result showed that chalcone1with the lowestIC 50 value is a potential candidate as an antimalarial agent.