Synthesis, Antimicrobial and Antioxidant Activity of Chalcone Derivatives Containing Thiobarbitone Nucleus

Abstract

In this paper we reported the synthesis of novel series of 5-[1,3-bis (4- substituted phenyl) prop-2-en-1-ylidene]- 2-thioxodihydropyrimidine-4,6(1H, 5H)-diones (5a-k). The target compounds were synthesized by the Knoevenagel condensation of different chalcones (3a-k) with thiobarbituric acid using acetic acid as a catalyst in ethanol. These compounds were screened for their antimicrobial and antioxidant activities. From antimicrobial activity results it was found that compounds 5e, 5i and 5k displayed good antibacterial and antifungal activity against all tested strains. Further, the selected compounds were studied for docking using the enzyme, Glucosamine-6-phosphate synthase and the compounds 5a, 5e and 5k have emerged as an active antimicrobial agents with least binding energy (-4.52 and -4.41 kJ mol-1). Compounds 5c and 5f showed promising free radical scavenging and Fe+2 ion chelating activity.