Abstract
Tuberculosis (TB) is of increasing concern due to the recent emergence and spread of MDR-TB, XDR-TB, TDR-TB and HIV/AIDS pandemic. There is urgent need for novel antitubercular agents which can shorten the treatment duration. Based on isosteric replacement and 3D structural similarity between Linezolid, an oxazolidine antimycobacterial agent, we have designed novel 4-amino-3,5-di(substituted)thiazolin-2(3H)thione/ones, synthesized and evaluated for their antimycobacterial activity on Mycobacterium tuberculosis H37Rv strain. Some of the compounds exhibited potent antimycobacterial activity with MIC values in the range of 1-2 µg/mL. Active compounds were further screened against MDR-TB and XDR-TB strain and found to exhibit promising in vitro activity.
Keywords: Antimycobacterial activity, MDR-TB, thiazolin-thione/ones, XDR-TB.
Anti-Infective Agents
Title:Synthesis and Antitubercular Activity of a Series of Thiazole Derivatives
Volume: 12 Issue: 2
Author(s): Mahesh Chhabria, Shailesh Patel, Sandeep Dholakia, Hardik Mistry and Sweta Patel
Affiliation:
Keywords: Antimycobacterial activity, MDR-TB, thiazolin-thione/ones, XDR-TB.
Abstract: Tuberculosis (TB) is of increasing concern due to the recent emergence and spread of MDR-TB, XDR-TB, TDR-TB and HIV/AIDS pandemic. There is urgent need for novel antitubercular agents which can shorten the treatment duration. Based on isosteric replacement and 3D structural similarity between Linezolid, an oxazolidine antimycobacterial agent, we have designed novel 4-amino-3,5-di(substituted)thiazolin-2(3H)thione/ones, synthesized and evaluated for their antimycobacterial activity on Mycobacterium tuberculosis H37Rv strain. Some of the compounds exhibited potent antimycobacterial activity with MIC values in the range of 1-2 µg/mL. Active compounds were further screened against MDR-TB and XDR-TB strain and found to exhibit promising in vitro activity.
Export Options
About this article
Cite this article as:
Chhabria Mahesh, Patel Shailesh, Dholakia Sandeep, Mistry Hardik and Patel Sweta, Synthesis and Antitubercular Activity of a Series of Thiazole Derivatives, Anti-Infective Agents 2014; 12 (2) . https://dx.doi.org/10.2174/22113525113119990119
DOI https://dx.doi.org/10.2174/22113525113119990119 |
Print ISSN 2211-3525 |
Publisher Name Bentham Science Publisher |
Online ISSN 2211-3533 |
Call for Papers in Thematic Issues
An Overview of Drugs for Multiple Targets and Variants of SARS-CoV-2 Through Artificial Intelligence, Machine Learning, Deep Learning, and Experimental Analysis
The emergence and rapid evolution of SARS-CoV-2 variants have posed significant challenges in the ongoing fight against the COVID-19 pandemic. The development of effective treatments for multiple viral targets and variants demands innovative approaches, including artificial intelligence (AI), machine learning (ML), and deep learning (DL) techniques. This special issue aims ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Bilayer Hydrophobic Thickness and Integral Membrane Protein Function
Current Protein & Peptide Science Fatty Acid Intakes and Coronary Heart Disease Mortality in Japan: NIPPON DATA90, 1990-2005
Current Nutrition & Food Science Antimicrobial Activity of Phenolics and Glucosinolate Hydrolysis Products and their Synergy with Streptomycin against Pathogenic Bacteria
Medicinal Chemistry Ligustrazine Derivatives. Part 8: Design, Synthesis, and Preliminary Biological Evaluation of Novel Ligustrazinyl Amides as Cardiovascular Agents
Medicinal Chemistry Editorial [Hot Topic: Structure Based Drug Design (Guest Editor: K.V. Radha Kishan)]
Current Protein & Peptide Science QSAR and the Prediction of T-Cell Epitopes
Current Proteomics Listeria monocytogenes as a Vector for Anti-Cancer Therapies
Current Gene Therapy Effect of Common NAT2 Variant Alleles in the Acetylation of the Major Clonazepam Metabolite, 7-minoclonazepam
Drug Metabolism Letters Recent Highlights on Molecular Hybrids Potentially Useful in Central Nervous System Disorders
Mini-Reviews in Medicinal Chemistry Molecular Docking and Dynamics Simulation Studies of a Dataset of NLRP3 Inflammasome Inhibitors
Recent Advances in Inflammation & Allergy Drug Discovery Potential Natural Antimycobacterial Metabolites from Some Sub-Saharan Medicinal Plants
Anti-Infective Agents Design, Synthesis and Biological Evaluation of Novel Fluorinated Heterocyclic Hybrid Molecules Based on Triazole & Quinoxaline Scaffolds Lead to Highly Potent Antimalarials and Antibacterials
Letters in Drug Design & Discovery Secondary Metabolites Derived from Actinomycetes: Iron Modulation and Their Therapeutic Potential
The Natural Products Journal The Lord of the Bacteria: The Fellowship of the Leader and Other Serine Protease Inhibitors
Current Pharmaceutical Design Tuberculosis: Current Treatment and New Drug Development
Anti-Infective Agents in Medicinal Chemistry Subject Index to Volume 1
Current Pharmacogenomics Hybridization Approach to Drug Discovery Inhibiting <i>Mycobacterium tuberculosis</i>-An Overview
Current Topics in Medicinal Chemistry Amyloidosis and Auto-Inflammatory Syndromes
Current Drug Targets - Inflammation & Allergy MIANN Models of Networks of Biochemical Reactions, Ecosystems, and U.S. Supreme Court with Balaban-Markov Indices
Current Bioinformatics Leishmaniasis: Prevention, Parasite Detection and Treatment
Current Medicinal Chemistry