Abstract
The title compounds have been synthesized and tested for structure activity relationship for Phospholipase A2 (PLA2) [E.C. 3.1.1.4] enzyme inhibition. The in vitro anti-tubercular, PLA2 enzyme inhibitory activities of azetidin-2-one derivatives and in vivo anti-inflammatory studies using mice are highlighted. The analogues of azetidin-2-one were prepared based on the initial activity against Mycobacterium tuberculosis (Mtb). Certain azetidin-2-one analogues described herein showed moderate to good anti-tubercular activity. In particular, two compounds (4f) and (4g) exhibited MIC values of 1.56 and 0.78 μg/mL respectively against the Mtb H37Rv strain. Chloro substitution on aryloxy acid apparently enhanced the antimycobacterial activity and also PLA2 inhibition in the azetidin-2-one series described herein. The ability of azetidin-2-one analogues as anti-inflammatory agents has also been determined. The results show some correlation between anti-inflammatory, anti-tubercular activity and expression of PLA2 enzyme.
Keywords: Phospholipase A2 (PLA2), anti-inflammatory, antitubercular, azetidin-2-one derivatives, mycobacterium tuberculosis(Mtb)
Medicinal Chemistry
Title: Anti-Tubercular and Anti-Inflammatory Activities of Azetidin-2-One Derivatives and Their Effects on the Activity of Phospholipase A2
Volume: 4 Issue: 2
Author(s): Mayur C. Yerigeri, Satish Kumar Murari, Kuntebommanahalli N. Thimmaiah, Shanta Kumar Sugur Math and Bannikuppe Sannanaik Vishwanath
Affiliation:
Keywords: Phospholipase A2 (PLA2), anti-inflammatory, antitubercular, azetidin-2-one derivatives, mycobacterium tuberculosis(Mtb)
Abstract: The title compounds have been synthesized and tested for structure activity relationship for Phospholipase A2 (PLA2) [E.C. 3.1.1.4] enzyme inhibition. The in vitro anti-tubercular, PLA2 enzyme inhibitory activities of azetidin-2-one derivatives and in vivo anti-inflammatory studies using mice are highlighted. The analogues of azetidin-2-one were prepared based on the initial activity against Mycobacterium tuberculosis (Mtb). Certain azetidin-2-one analogues described herein showed moderate to good anti-tubercular activity. In particular, two compounds (4f) and (4g) exhibited MIC values of 1.56 and 0.78 μg/mL respectively against the Mtb H37Rv strain. Chloro substitution on aryloxy acid apparently enhanced the antimycobacterial activity and also PLA2 inhibition in the azetidin-2-one series described herein. The ability of azetidin-2-one analogues as anti-inflammatory agents has also been determined. The results show some correlation between anti-inflammatory, anti-tubercular activity and expression of PLA2 enzyme.
Export Options
About this article
Cite this article as:
Yerigeri C. Mayur, Murari Kumar Satish, Thimmaiah N. Kuntebommanahalli, Sugur Math Kumar Shanta and Vishwanath Sannanaik Bannikuppe, Anti-Tubercular and Anti-Inflammatory Activities of Azetidin-2-One Derivatives and Their Effects on the Activity of Phospholipase A2, Medicinal Chemistry 2008; 4 (2) . https://dx.doi.org/10.2174/157340608783789149
DOI https://dx.doi.org/10.2174/157340608783789149 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...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
Related Articles
-
Identification and in silico Characterization of Semenogelin II Protein in Semen- A Marker for Diagnosis of male Infertility
Current Proteomics Imidazole and 1,2,4-Triazole-based Derivatives Gifted with Antitubercular Activity: Cytotoxicity and Computational Assessment
Current Topics in Medicinal Chemistry Small Ruminant Lentiviruses and Human Immunodeficiency Virus: Cousins that Take a Long View
Current HIV Research Ligustrazine Derivatives. Part 8: Design, Synthesis, and Preliminary Biological Evaluation of Novel Ligustrazinyl Amides as Cardiovascular Agents
Medicinal Chemistry HPLC as a Tool in Medicinal Chemistry for the Monitoring of Tricyclic Antidepressants in Biofluids
Mini-Reviews in Medicinal Chemistry New Pyrrole Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics
Letters in Drug Design & Discovery Asthma and High Altitude: Is It Safe to Be and Work?
Current Respiratory Medicine Reviews Short Antimicrobial Peptides
Recent Patents on Anti-Infective Drug Discovery pH-dependent Activities and Structural Stability of Loop-2-anchoring Helix of RadA Recombinase from Methanococcus voltae
Protein & Peptide Letters Inhalation Delivery of Protein Therapeutics
Inflammation & Allergy - Drug Targets (Discontinued) Protein Microarrays for Studies of Drug Mechanisms and Biomarker Discovery in the Era of Systems Biology
Current Pharmaceutical Design Novel Antibacterial Agents: An Emergent Need to Win the Battle Against Infections
Mini-Reviews in Medicinal Chemistry Defining ‘Satisfactory Response’ to Therapy in Abdominal Tuberculosis: A Work in Progress
Infectious Disorders - Drug Targets Study of Parasitic Infections, Cancer, and other Diseases with Mass-Spectrometry and Quantitative Proteome-Disease Relationships
Current Proteomics Using QM/MM Methods for the Exploration of Electron Transfer Pathways
Current Inorganic Chemistry (Discontinued) High Throughput Crystallography of TB Drug Targets
Infectious Disorders - Drug Targets Development of Aminoglycoside Antibiotics by Carbohydrate Chemistry
Mini-Reviews in Medicinal Chemistry Meet Our Executive Editor
Current HIV Research Hybridization Approach to Drug Discovery Inhibiting <i>Mycobacterium tuberculosis</i>-An Overview
Current Topics in Medicinal Chemistry Association of Serum Malondialdehyde and C-reactive Protein Levels with Exacerbations of Chronic Obstructive Pulmonary Disease
Current Respiratory Medicine Reviews