1282522-71-7Relevant academic research and scientific papers
Advent of imidazo[1,2-a]pyridine-3-carboxamides with potent multi- and extended drug resistant antituberculosis activity
Moraski, Garrett C.,Markley, Lowell D.,Hipskind, Philip A.,Boshoff, Helena,Cho, Sanghyun,Franzblau, Scott G.,Miller, Marvin J.
, p. 466 - 470 (2011/08/22)
A set of nine 2,7-dimethylimidazo[1,2-a]pyridine-3-carboxamides and one 2,6-dimethylimidazo[1,2-a]pyrimidine-3-carboxamide were synthesized. The compounds were evaluated for their in vitro antituberculosis activity versus replicating, nonreplicating, multi- and extensive drug resistant Mtb strains. The MIC90 values of seven of these agents were ≤1 μM against the various tuberculosis strains tested. A representative compound of this class (1) was screened against seven nontubercular strains as well as other nonmycobacteria organisms and demonstrated remarkable microbe selectivity. A transcriptional profiling experiment of Mtb treated with compound 1 was performed to give a preliminary indication of the mode of action. Lastly, the in vivo ADME properties of compounds 1, 3, 4, and 6 were assessed. The 2,7-dimethylimidazo[1,2-a]pyridine-3-carboxamides are a druglike and synthetically accessible class of anti-TB agents that have excellent selective potency against multi- and extensive drug resistant TB and encouraging pharmacokinetics.
