Design and Synthesis of Bis-pyrimidines Linked with Thiazolidin-4-one as New Antibacterial Agents

Abstract

A series of novel 3-4-[2-hydroxy-5-(4-hydroxy-3-2-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-6-phenyl-4-pyrimidinylbenzyl)phenyl]-6-phenyl-2-pyrimidinyl-2-(aryl)-1,3-thiazolan-4-ones 5(a-j) have been synthesized and assayed for their antibacterial activity against B. subtilis, B. sphaericus, S. aureus, P. aeruginosa, K. Aerogenes and C. violaceum. The inhibition zones and minimal inhibitory concentrations were measured and compared with the streptomycin. The antibacterial screening data reveal that the compounds containing 4-nitrophenyl (5c), 3-nitrophenyl (5d), 4-dimethylaminophenyl (5g) and 1,3-benzodioxole (5j) moiety at 2-position of the thiazolidin-4-one ring exhibited potent inhibitory activity towards all the tested microorganism, which is higher than streptomycin. The other compounds also showed moderate to good activity.

Untitled

“…Given the biological profile of flavones and tetrazole derivatives and our work on synthesizing new heterocyclic compounds [19][20][21][22] , we designed a set of hybrid molecules with different heterocyclic scaffolds, such as flavone and tetrazole intending to increase their antimicrobial activities. In the present study, we report the synthesis of new series of 2phenyl-3-(1-aryl-1H-1, 2, 3, 4-tetraazol-5-yl)-4H-4chromenone 11(a-j) and evaluation of their in-vitro antimicrobial activities.…”