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 1 was synthesized from 2,4-dihydroxyacetophenone and 4-metoxybenzaldehyde as starting materials using base catalyst KOH via Claisen-Schmidt Condensation. The synthesis flavone 2 was carried out by cyclization of chalcone 1 using I2 in DMSO, while the flavanone 3 was produced by cyclization of chalcone 1 using NaOAc as a base catalyst. An in vitro antimalarial activity of the compound 1, 2 and 3 have 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 IC50 value of compound 1, 2, 3 and a positive control were 0.25; 0.62; 1.33 and 0.35 mM, respectively. The result showed that chalcone 1 with the lowest IC50 value is a potential candidate as an antimalarial agent. © 2019 Trans Tech Publications Ltd, Switzerland.