Abstract
The conjugation of different substituted styryl (-CH=CH-Aryl) moieties with the biologically relevant heteroaromatic scaffolds such as 4-benzylidene-2-methyloxazol-5-one, 3-methyl-1-phenylpyrazol-5-one, 2-methylbenzimidazole, 6-methyluracil afforded the newer series (four different series, 1A-3C, 2A-C, 3A-C & 4A-C) of styrene derivatives. Newer styrene derivatives were synthesized and characterized by IR, NMR (1H & 13C), Mass spectroscopic/spectrometric methods and elemental analysis. Results of the antibacterial activity study reveal that the synthesized compounds possess in-vitro activity against the tested bacterial strains, which, however, was comparatively very less than that of the standard drug, amikacin sulphate. From the structure-activity relationship study, it could be attributed that the overall antibacterial efficacy of the conjugated series of styrene derivatives is the sum of bio-effectiveness of styryl moieties and heterocyclic scaffolds.
Keywords: Antibacterial, benzimidazole, oxazole, pyrazole, styryl, uracil.
Anti-Infective Agents
Title:Synthesis and Evaluation of Heterocyclic Scaffold-Based Styrene Conjugates as New Antibacterial Agents
Volume: 12 Issue: 2
Author(s): M. Rudrapal, T. Mariya Babu, T. Ravi Chandra, U. Divya Durga, V. Swathi, B. Usha Naga Chandrika and K. Ravishankar
Affiliation:
Keywords: Antibacterial, benzimidazole, oxazole, pyrazole, styryl, uracil.
Abstract: The conjugation of different substituted styryl (-CH=CH-Aryl) moieties with the biologically relevant heteroaromatic scaffolds such as 4-benzylidene-2-methyloxazol-5-one, 3-methyl-1-phenylpyrazol-5-one, 2-methylbenzimidazole, 6-methyluracil afforded the newer series (four different series, 1A-3C, 2A-C, 3A-C & 4A-C) of styrene derivatives. Newer styrene derivatives were synthesized and characterized by IR, NMR (1H & 13C), Mass spectroscopic/spectrometric methods and elemental analysis. Results of the antibacterial activity study reveal that the synthesized compounds possess in-vitro activity against the tested bacterial strains, which, however, was comparatively very less than that of the standard drug, amikacin sulphate. From the structure-activity relationship study, it could be attributed that the overall antibacterial efficacy of the conjugated series of styrene derivatives is the sum of bio-effectiveness of styryl moieties and heterocyclic scaffolds.
Export Options
About this article
Cite this article as:
Rudrapal M., Babu Mariya T., Chandra Ravi T., Durga Divya U., Swathi V., Chandrika Usha Naga B. and Ravishankar K., Synthesis and Evaluation of Heterocyclic Scaffold-Based Styrene Conjugates as New Antibacterial Agents, Anti-Infective Agents 2014; 12 (2) . https://dx.doi.org/10.2174/2211352512666140715165318
DOI https://dx.doi.org/10.2174/2211352512666140715165318 |
Print ISSN 2211-3525 |
Publisher Name Bentham Science Publisher |
Online ISSN 2211-3533 |
- 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
-
Serial Analysis of Gene Expression in Eukaryotic Pathogens
Infectious Disorders - Drug Targets Proteomics on Fixed Tissue Specimens – A Review
Current Proteomics Mechanism of Action of Limonene in Tumor Cells: A Systematic Review and Meta-Analysis
Current Pharmaceutical Design Imaging in Inflammatory Bowel Disease Mucosal Healing in Ulcerative Colitis: Relevance for Clinical Outcomes
Current Drug Targets Tea Consumption and Risk of Ischemic Stroke: a Brief Review of the Literature
Current Pharmaceutical Biotechnology A Highly Concentrated and Taste-Improved Aqueous Formulation of Efavirenz for a More Appropriate Pediatric Management of the Anti-HIV Therapy
Current HIV Research Synthesis of 1,8-Dioxo-Decahydroacridines using Pyridinium Hydrogen Sulfate Ionic Liquid as an Green, Efficient and Reusable Catalyst
Letters in Organic Chemistry A Liver-Derived Rat Epithelial Cell Line from Biliary Origin Acquires Hepatic Functions Upon Sequential Exposure to Hepatogenic Growth Factors and Cytokines
Current Medicinal Chemistry Addressing the Challenge: Current and Future Directions in Ovarian Cancer Therapy
Current Gene Therapy Overlapping Ligand Specificity of P-Glycoprotein and Serum α1-Acid Glycoprotein:Evidences and Potential Implications
Current Drug Metabolism Chemometric Evaluation of the Significance of Molecular Structural Descriptors on Binding of Acridinone Derivatives to DNA
Letters in Drug Design & Discovery In Vitro Cytotoxicity Evaluation of Some Substituted Indazole Derivatives
Letters in Drug Design & Discovery Natural Products in Drug Discovery - Concepts and Approaches for Tracking Bioactivity
Current Organic Chemistry Nanomedicine: Potential Devices for Diagnostics
Recent Patents on Nanomedicine Metal Release from and Sequestration by Metallothioneins Monitored by Electrochemistry and SPR
Current Pharmaceutical Biotechnology From Body Art to Anticancer Activities: Perspectives on Medicinal Properties of Henna
Current Drug Targets Development of Electrochromic Devices
Recent Patents on Nanotechnology Pharmacological Potentials and Nutritional Values of Tropical and Subtropical Fruits of India: Emphasis on their Anticancer Bioactive Components
Recent Patents on Anti-Cancer Drug Discovery ADAM8/MS2/CD156, an Emerging Drug Target in the Treatment of Inflammatory and Invasive Pathologies
Current Pharmaceutical Design Interactions of Curcumin and Its Derivatives with Nucleic Acids and their Implications
Mini-Reviews in Medicinal Chemistry