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
-
Antimycobacterial Activity: Synthesis and Biological Evaluation of Novel Substituted (3E,5E)-3,5-diarylidene-1-phenethylpiperidine-4-one Derivatives
Letters in Drug Design & Discovery Structural and Functional Properties of NAD Kinase, a Key Enzyme in NADP Biosynthesis
Mini-Reviews in Medicinal Chemistry Ultrasonic and Microwave Assisted Synthesis of Nitrogen-Containing Derivatives of Juglone as Potential Antibacterial Agents
Letters in Organic Chemistry A Dilemma of Functional Genomics: Count the Chickens or Study their Eggs ?
Current Genomics Methods to Measure Target Site Penetration of Antibiotics in Critically Ill Patients
Current Clinical Pharmacology Enhanced Efficacy of DNA Vaccines Against an Intracellular Bacterial Pathogen by Genetic Adjuvants
Current Pharmaceutical Biotechnology Psoriatic Arthritis – Review of the Immunologic, Clinic and Therapeutic Aspects of an Inflammatory Systemic Disease
Current Rheumatology Reviews Marine Actinomycetes-derived Natural Products
Current Topics in Medicinal Chemistry Editorial (Thematic Issue: Nanotechnology for Drug Delivery Applications)
Current Drug Delivery Association of N-Acetyltransferase-2 Genotypes and Anti-Tuberculosis Induced Liver Injury: First Case-Controlled Study from Iran
Current Drug Safety Effects of Chrisotherapeutic Gold Compounds on Prostaglandin E2 Production
Current Drug Targets - Inflammation & Allergy Patent Selections
Recent Patents on Anti-Infective Drug Discovery Virtual Screening of Drugs: Score Functions, Docking, and Drug Design
Current Computer-Aided Drug Design The Beneficial Role of Vitamin D in Human Immunodeficiency Virus Infection
Current HIV Research Angiogenin as a Molecular Target for the Treatment of Prostate Cancer
Current Cancer Therapy Reviews Gold Nanoparticles - Synthesis and Applications in Cancer Management
Recent Patents on Materials Science Antimicrobial Compounds from Marine Invertebrates-Derived Microorganisms
Current Medicinal Chemistry Ligand-Receptor Communication and Drug Design
Current Protein & Peptide Science Neopterin as a Marker for Immune System Activation
Current Drug Metabolism Simultaneously Determining Seven Second-Line Anti-TB Drugs by UHPLC- MS: Application for TDM in HIV-TB Patients
Current Pharmaceutical Analysis