Novel 5-Nitrofuran-Tagged Imidazo-Fused Azines and Azoles Amenable by the Groebke-Blackburn-Bienayme Multicomponent Reaction: Activity Profile against ESKAPE Pathogens and Mycobacteria.

ABSTRACT: A chemically diverse set of 13 5-nitrofuran-tagged heterocyclic compounds has been prepared via the Groebke-Blackburn-Bienaymé multicomponent reaction. The testing of these compounds against the so-called ESKAPE panel of pathogens identified an apparent lead compound-N-cyclohexyl-2-(5-nitrofuran-2-yl)imidazo[1,2-a]pyridine-3-amine (4a)-which showed an excellent profile against Enterobacter cloacae, Staphylococcus aureus, Klebsiella pneumoniae, and Enterococcus faecalis (MIC 0.25, 0.06, 0.25 and 0.25 µg/mL, respectively). Its antibacterial profile and practically convenient synthesis warrant further pre-clinical development. Certain structure-activity relationships were established in the course of this study which were rationalized by the flexible docking

SUBMITTER: Sapegin A 

PROVIDER: S-EPMC9496245 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature