Antibacterial activities of Groebke-Blackburn-Bienayme-derived imidazo[1,2-a]pyridin-3-amines.

ABSTRACT: We sought to explore the imidazo[1,2-a]pyridin-3-amines for TLR7 (or 8)-modulatory activities. This chemotype, readily accessed via the Groebke-Blackburn-Bienaymé multi-component reaction, resulted in compounds that were TLR7/8-inactive, but exhibited bacteriostatic activity against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). To investigate the mechanism of antibacterial activity of this new chemotype, a resistant strain of S. aureus was generated by serially passaging the organism in escalating doses of the most active analogue. A comparison of minimum inhibitory concentrations (MICs) of known bacteriostatic agents in wild-type and resistant strains indicates a novel mechanism of action. Structure-activity relationship studies have led to the iden

SUBMITTER: Shukla NM 

PROVIDER: S-EPMC3448811 | biostudies-literature | 2012 Oct

REPOSITORIES: biostudies-literature