Synthesis and antibacterial evaluation of new pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-one hybrids linked to different heteroarene units

A three-component protocol involving the reaction of 3-aminothieno[2,3-b]pyridine-2-carboxylate, Me2NCH(OMe)(2) and heteroaryl (bis)amines in dioxane under microwave irradiation yielded a new series of pyrimidinones. The target hybrids were formed by an initial formamidine formation, followed by cross-imidination and [5+1] heterocyclization. Pyrazole-linked pyrimidinones displayed the best antibacterial activity against all the gram-positive and negative strains tested.

Automated summary

A three-component protocol was used to synthesize a new series of pyrimidinones, with pyrazole-linked pyrimidinones displaying the best antibacterial activity against both gram-positive and negative strains.