Abstract
A series of twelve novel azetedinones 4a-l have been synthesized by cyclocondensation of various Schiff bases of amino thiadiazole with chloroacetyl chloride in the presence of triethylamine. Various novel Schiff bases 3a-l were synthesized by condensation of 2-amino-5-aryl-5H-thiazolo[4,3-b]-l,3,4-thiadiazole with various aryl aldehydes. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR and mass spectra. The titled compounds 3a-l and 4a-l were evaluated for anti-tubercular activity at a concentration of 0.1-100 μg/mL by Microplate Blue Alamar Assay method. Azetedinones 4a-l showed very good inhibition against the growth of Mycobacterium tuberculosis compared to compounds 3a-l and standard Streptomycin and Pyrazinamide.
Keywords: 2-amino-5-aryl-5H-thiazolo[4, 3-b]-1, 3, 4-thiadiazoles, Antitubercular activity, Azetidin-2-ones, Schiff base
Letters in Drug Design & Discovery
Title:Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents
Volume: 9 Issue: 6
Author(s): M. Himaja, Asif Karigar, M. V. Ramana, D. Munirajasekhar and Mukesh S. Sikarwar
Affiliation:
Keywords: 2-amino-5-aryl-5H-thiazolo[4, 3-b]-1, 3, 4-thiadiazoles, Antitubercular activity, Azetidin-2-ones, Schiff base
Abstract: A series of twelve novel azetedinones 4a-l have been synthesized by cyclocondensation of various Schiff bases of amino thiadiazole with chloroacetyl chloride in the presence of triethylamine. Various novel Schiff bases 3a-l were synthesized by condensation of 2-amino-5-aryl-5H-thiazolo[4,3-b]-l,3,4-thiadiazole with various aryl aldehydes. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR and mass spectra. The titled compounds 3a-l and 4a-l were evaluated for anti-tubercular activity at a concentration of 0.1-100 μg/mL by Microplate Blue Alamar Assay method. Azetedinones 4a-l showed very good inhibition against the growth of Mycobacterium tuberculosis compared to compounds 3a-l and standard Streptomycin and Pyrazinamide.
Export Options
About this article
Cite this article as:
Himaja M., Karigar Asif, V. Ramana M., Munirajasekhar D. and S. Sikarwar Mukesh, Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents, Letters in Drug Design & Discovery 2012; 9 (6) . https://dx.doi.org/10.2174/157018012800673038
DOI https://dx.doi.org/10.2174/157018012800673038 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
Related Articles
-
β-Carboline Alkaloids: Biochemical and Pharmacological Functions
Current Medicinal Chemistry Key Targets and Relevant Inhibitors for the Drug Discovery of Tuberculosis
Current Drug Targets subject Index To Volume 2
Current Drug Targets - Infectious Disorders Oxidative Stress and Antioxidant Potential of One Hundred Medicinal Plants
Current Topics in Medicinal Chemistry Therapeutic Use of Snake Venom Components: A Voyage from Ancient to Modern India
Mini-Reviews in Organic Chemistry Tofacitinib, an Oral Janus Kinase Inhibitor: Perspectives in Dermatology
Current Medicinal Chemistry Lignans and Neolignans Anti-tuberculosis Identified by QSAR and Molecular Modeling
Combinatorial Chemistry & High Throughput Screening Role of Genetic Interactions in Lung Diseases Detection Using Computational Approaches: A Review
Current Chinese Computer Science Fluoroquinolones as Chemotherapeutics Against Mycobacterial Infections
Current Pharmaceutical Design Editorial (Thematic Issue: Molecular Determinants of Bacterial Diseases)
Current Medicinal Chemistry Nanoemulsion Formulation Enhances Intracellular Activity of Capuramycin Analogues against Mycobacterium Tuberculosis
Drug Delivery Letters Sepsis: Links between Pathogen Sensing and Organ Damage
Current Pharmaceutical Design Current Research Issues in the Pharmacokinetics of Antiretroviral Drugs in Children
Current Pediatric Reviews Behcets Syndrome: Literature Review
Current Rheumatology Reviews Dried Blood Spots: A New Tool for Tuberculosis Treatment Optimization
Current Pharmaceutical Design Polyfunctional Antibiotics Affecting Bacterial Membrane Dynamics
Anti-Infective Agents in Medicinal Chemistry Vitamin D in COPD - A Pleiotropic Micronutrient in a Multisystem Disease
Current Respiratory Medicine Reviews Nanoparticles vs Cancer: A Multifuncional Tool
Current Topics in Medicinal Chemistry Nano-carriers for the Treatment of Tuberculosis
Recent Patents on Anti-Infective Drug Discovery Deubiquitinating Enzymes as Promising Drug Targets for Infectious Diseases
Current Pharmaceutical Design