Related Experiment Video
Updated: Sep 28, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Quinoline derivatives as potential anti-tubercular agents: Synthesis, molecular docking and mechanism of action
Chun-Xiu Liu1, Xin Zhao1, Lei Wang1
1College of Pharmacy, Guizhou University, Guiyang, 550025, PR China.
Abstract:
Development of new drugs with novel mechanisms of action is required to combat the problem of drug-resistant Mycobacterium tuberculosis. The present investigation is aimed at combining two pharmacophores (quinoline or isoquinolines and thiosemicarbazide) to synthesize a series of compounds. Seven compounds were synthesized based on combination principle in this study. The compound 1-7 showed activities against M. tuberculosis H37Rv strain with MIC values rang from 2 to 8 μg/ml. Compound 5 exhibited remarkable antimycobacterial activity (MIC = 2 μg/ml), and was therefore selected for study of the mechanism of action. Molecular docking suggested initially that compound 5 could occupy the active site of KatG of M. tuberculosis. Furthermore compound 5 exhibited potent inhibitory effect on activity of KatG. RT-PCR finally displayed that compound 5 could up-regulate the transcription of katG of M. tuberculosis. Together, these studies reveal that compound 5 might be the inhibitor of KatG of Mycobacterium tuberculosis. One of the more significant findings to emerge from this study is that KatG of M.tuberculosis can be used as a putative novel target for new anti-tubercular drug design.
More Related Videos
10:29Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
09:57System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
Related Concept Videos
Drugs that Destabilize Microtubules
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Antihypertensive Drugs: Thiazide-Class Diuretics
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Drug Discovery: Overview