title: Synthesis and structure activity relationship of imidazo[1,2-a]pyridine-8-carboxamides as a novel antimycobacterial lead series.
abstract: Imidazo[1,2-a]pyridine-8-carboxamides as a novel antimycobacterial lead were generated by whole cell screening of a focused library against Mycobacterium tuberculosis. Herein, we describe the synthesis and structure activity relationship evaluation of this class of inhibitors and the optimization of physicochemical properties. These are selective inhibitors of Mycobacterium tuberculosis with no activity on either gram positive or gram negative pathogens.
authors.affiliation: Department of Medicinal Chemistry, AstraZeneca India Pvt Ltd, Avishkar, Bellary Road, Hebbal, Bangalore 560024, India. sreekanth.ramachandran@astrazeneca.com
authors.forename: Sreekanth
authors.initials: S
authors.lastname: Ramachandran
authors.forename: Manoranjan
authors.initials: M
authors.lastname: Panda
authors.forename: Kakoli
authors.initials: K
authors.lastname: Mukherjee
authors.forename: Nilanjana Roy
authors.initials: NR
authors.lastname: Choudhury
authors.forename: Subramanyam J
authors.initials: SJ
authors.lastname: Tantry
authors.forename: Chaitanya Kumar
authors.initials: CK
authors.lastname: Kedari
authors.forename: Vasanthi
authors.initials: V
authors.lastname: Ramachandran
authors.forename: Sreevalli
authors.initials: S
authors.lastname: Sharma
authors.forename: V K
authors.initials: VK
authors.lastname: Ramya
authors.forename: Supreeth
authors.initials: S
authors.lastname: Guptha
authors.forename: Vasan K
authors.initials: VK
authors.lastname: Sambandamurthy
mesh_terms: D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000995:Antitubercular Agents / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy
chemical_list: D000577:Amides; D000995:Antitubercular Agents; D011725:Pyridines; C001439:imidazo(1,2-a)pyridine
keywords: Antimycobacterial activity; Physicochemical properties; Structure activity relationship; Whole cell screening