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  • Title: Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives.
    Author: Lv K, Li L, Wang B, Liu M, Wang B, Shen W, Guo H, Lu Y.
    Journal: Eur J Med Chem; 2017 Sep 08; 137():117-125. PubMed ID: 28577507.
    Abstract:
    We report herein the design and synthesis of "novel imidazo [1,2-a]pyridine-3-carboxamides (IPAs)" bearing a variety of different linkers, based on the structure of IMB-1402 discovered in our lab. Results reveal that 2,6-dimethyl-N-[2-(phenylamino)ethyl] IPAs with an electron-donating group on the benzene ring as a potent scaffold. Compounds 26g and 26h have considerable activity (MIC: 0.041-2.64 μM) against drug-sensitive/resistant MTB strains, and they have acceptable safety indices against MTB H37Rv with the SI values of 4395 and 1405, respectively. Moreover, N-[2-(piperazin-1-yl)ethyl] moiety was also identified as a potentially alternative linker (compound 31), opening a new direction for further SAR studies.
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