Identification of <i>N</i>-(2-Phenoxyethyl)imidazo[1,2-<i>a</i>]pyridine-3-carboxamides as New Antituberculosis Agents

Abstract

A series of imidazo[1,2-<i>a</i>]pyridine carboxamides (IPAs) bearing an <i>N</i>-(2-phenoxyethyl) moiety was designed and synthesized as new antitubercular agents. Seven 2,6-dimethyl IPAs demonstrated excellent <i>in vitro</i> activity (MIC: 0.025-0.054 μg/mL) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistant <i>Mycobacterium tuberculosis</i>strains. Compound <b>10j</b> displayed acceptable safety and pharmacokinetic properties, opening a new direction for further development.