title: Identification ofN-(2-Phenoxyethyl)imidazo[1,2-a]pyridine-3-carboxamides as New Antituberculosis Agents.
abstract: A series of imidazo[1,2-a]pyridine carboxamides (IPAs) bearing anN-(2-phenoxyethyl) moiety was designed and synthesized as new antitubercular agents. Seven 2,6-dimethyl IPAs demonstrated excellentin vitroactivity (MIC: 0.025-0.054 μg/mL) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistantMycobacterium tuberculosisstrains. Compound10jdisplayed acceptable safety and pharmacokinetic properties, opening a new direction for further development.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050, China.
authors.forename: Zhaoyang
authors.initials: Z
authors.lastname: Wu
authors.affiliation: Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University , Beijing 101149, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Lu
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050, China.
authors.forename: Linhu
authors.initials: L
authors.lastname: Li
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050, China.
authors.forename: Rui
authors.initials: R
authors.lastname: Zhao
authors.affiliation: Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University , Beijing 101149, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Wang
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Department of Chemistry, Purdue University, West Lafayette, Indiana 47907, United States.
authors.forename: Kai
authors.initials: K
authors.lastname: Lv
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050, China.
authors.forename: Mingliang
authors.initials: M
authors.lastname: Liu
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050, China.
authors.forename: Xuefu
authors.initials: X
authors.lastname: You
keywords: Antitubercular agents; MTB H37Rv; N-(2-phenoxyethyl)imidazo[1,2-a]pyridine carboxamides; multidrug resistant-MTB; structure−activity relationship