Literature DB >> 23867166

Synthesis and structure activity relationship of imidazo[1,2-a]pyridine-8-carboxamides as a novel antimycobacterial lead series.

Sreekanth Ramachandran1, Manoranjan Panda, Kakoli Mukherjee, Nilanjana Roy Choudhury, Subramanyam J Tantry, Chaitanya Kumar Kedari, Vasanthi Ramachandran, Sreevalli Sharma, V K Ramya, Supreeth Guptha, Vasan K Sambandamurthy.   

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.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antimycobacterial activity; Physicochemical properties; Structure activity relationship; Whole cell screening

Mesh:

Substances:

Year:  2013        PMID: 23867166     DOI: 10.1016/j.bmcl.2013.06.043

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  The tuberculosis drug discovery and development pipeline and emerging drug targets.

Authors:  Khisimuzi Mdluli; Takushi Kaneko; Anna Upton
Journal:  Cold Spring Harb Perspect Med       Date:  2015-01-29       Impact factor: 6.915

2.  Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.

Authors:  Garrett C Moraski; Allen G Oliver; Lowell D Markley; Sanghyun Cho; Scott G Franzblau; Marvin J Miller
Journal:  Bioorg Med Chem Lett       Date:  2014-05-28       Impact factor: 2.823

3.  Design, synthesis, and biological evaluation of novel imidazo[1,2-a]pyridinecarboxamides as potent anti-tuberculosis agents.

Authors:  Oluseye K Onajole; Shichun Lun; Young Ju Yun; Damkam Y Langue; Michelle Jaskula-Dybka; Adrian Flores; Eriel Frazier; Ashle C Scurry; Ambernice Zavala; Karen R Arreola; Bryce Pierzchalski; A Jean-Luc Ayitou; William R Bishai
Journal:  Chem Biol Drug Des       Date:  2020-07-09       Impact factor: 2.817

  3 in total

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