N-(2-Phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides containing various amine moieties: Design, synthesis and antitubercular activity

Publication date: Available online 17 July 2019Source: Chinese Chemical LettersAuthor(s): Linhu Li, Apeng Wang, Bin Wang, Mingliang Liu, Kai Lv, Zeyu Tao, Chao Ma, Xican Ma, Bing Han, Aoyu Wang, Yu LuABSTRACTSeven 2,6-disubstituted N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamide series containing various amine moieties were designed and synthesized as new anti-TB agents. Many of them show excellent in vitro activity against both drug-sensitive MTB strain H37Rv and two MDR-MTB clinical isolates (MIC: < 0.002–0.030 μg/mL). Compounds 2f, 5e and 5 g display acceptable safety and pharmacokinetic profiles, opening a new direction for further development.Graphical AbstractSeven series were designed, synthesized and evaluated based on the lead WZY02 discovered by our lab. Compounds 2f, 5e and 5 g were found to have excellent in vitro anti-TB activity, acceptable safety and pharmacokinetic profiles.

Source: Chinese Chemical Letters - July 19, 2019 Category: Chemistry Source Type: research