DOI: 10.21276/sajp.2019.8.8.9

Pages: 436-442

Chalcone, its 4-methoxy, 4-methoxy-4,6-diphenyl-2-thiopyrimidine derivatives and chalcone epoxides were synthesized using the Claisen-Schmidt condensation between benzaldehyde derivatives and acetophenone at very low temperature in the presence of KOH and ethanol. Further cyclization reaction with thiourea gave the heterocyclic derivative. The melting points, actual yield, percentage yields and RF values of all the synthesized compounds were determined and their physical appearances recorded. The structures of the compounds were determined using FTIR, 1 H, 13C NMR experiments. The compounds were screened for in-vivo anti-inflammatory activity at the dose of 1mg/kg, 2mg/kg and 4mg/kg using egg albumin-induced paw oedema in rat. Diclofenac, 2mg/kg was used as the reference drug. The synthesized compounds were also subjected to in-vitro antimicrobial screening against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, and Candida albican. Ciprofloxacin, gentamycin and ketoconazole were used as reference standards. The compounds showed no antimicrobial activity but the 4- methoxy-4, 6-diphenyl-2-thiopyrimidne displayed remarkable anti-inflammatory activity. Keywords: Chalcones, Claisen-Schmidt condensation, Anti-inflammatory, Antifungal, Cnalcone epoxides, Heterocycles.