One-pot synthesis and biological evaluation of N-fused imidazoles as antibacterial agents and bacterial topoisomerase inhibitors

A series of N -fused imidazoles related to known inhibitors of human topoisomerase IIα were rapidly synthesized by a multicomponent GBB reaction under environmentally friendly conditions with microwave heating. Two of the compounds synthesized exhibited bacteriostatic activity against methicillin-resistant Staphylococcus aureus (MRSA) and other gram-positive bacteria, but none showed significant inhibition of bacterial topoisomerase. • A series of prospective bacterial topoisomerase inhibitors were synthesized • 30 (17 novel) compounds were prepared using a one-step method • Some compounds showed bacteriostatic activity, but none inhibited bacterial topoisomerase.