Related Experiment Video

Updated: Apr 20, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

Synthesis, molecular docking and anti-mycobacterial evaluation of new imidazo[1,2-a]pyridine-2-carboxamide

Gilish Jose¹, T H Suresha Kumara², Gopalpur Nagendrappa¹

¹Postgraduate Department of Chemistry, Jain University, 52 Bellary Road, Hebbal, Bangalore, Karnataka 560024, India.

European Journal of Medicinal Chemistry

|December 3, 2014

Abstract:

New anti-tubercular agents, imidazo[1,2-a]pyridine-2-carboxamide derivatives (5a-q) have been designed and synthesized. The structural considerations of the designed molecules were further supported by the docking study with a long-chain enoyl-acyl carrier protein reductase (InhA). The chemical structures of the new compounds were characterized by IR, (1)H NMR, (13)C NMR, HRMS and elemental analysis. In addition, single crystal X-ray diffraction has also been recorded for compound 5f. Compounds were evaluated in vitro against Mycobacterium tuberculosis H37Rv, and cytotoxicity against HEK-293T cell line. Amongst the tested compounds 5j, 5l and 5q were emerged as good anti-tubercular agents with low cytotoxicity. The structure-anti TB activity relationship of these derivatives was explained by molecular docking.

Keywords:

Anti-mycobacterial activity Imidazopyridine amide InhA Tuberculosis X-ray crystallography

More Related Videos

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

Published on: June 23, 2019

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

Related Concept Videos

Inhibitors of Bacterial DNA Synthesis

Inhibitors of Bacterial DNA Synthesis

Bacterial pathogens depend on precise and efficient DNA replication to sustain infection. Two type II topoisomerases—DNA gyrase and topoisomerase IV—are critical to this process, as they resolve DNA supercoiling and unlink chromosomes during replication. Fluoroquinolones, synthetic derivatives of quinolones, exploit this mechanism by stabilizing the transient DNA–enzyme cleavage complex, preventing strand religation, and causing lethal double-strand breaks. These...

Articles linked to this work by shared authors, journal, and citation graph.

A green and expedient synthesis of [1, 3] oxazine derivatives and their biological evaluation as a potent anti-tubercular and anti-microbial agent.

Bioorganic chemistry·2026

Flexible Electrochemical Biosensor for Non-Invasive, on-Site Cortisol Monitoring in Sweat and Saliva.

ACS measurement science au·2026

2-Aminothiophene and 2-aminothiazole scaffolds as potent antimicrobial agents: Design, synthesis, biological evaluation, and computational insights.

Bioorganic chemistry·2026

Synthesis, Characterization, Crystal Structure and Anti-TB and Anticancer Applications of Redox Active Phenanthroline Derivatized With Methyl-, Ethyl-, and Benzyl Carbazates.

Chemistry, an Asian journal·2026

Design, Synthesis, Biological Evaluation, and In Silico Studies of New Nitazoxanide Derivatives: Toward Broad-Spectrum Antimicrobial Agents.

Archiv der Pharmazie·2025

Structure-based design, synthesis, computational screening and biological evaluation of novel pyrrole fused pyrimidine derivatives targeting InhA enzyme.

RSC advances·2025

See all related articles