Abstract
Background: Many 2-substituted quinolines and especially 2-arylvinyl derivatives isolated from plants or prepared by synthesis have been designed from ethnopharmacological studies.
Objective: In order to explore new aspects of the structure-antituberculosis activity relationship, a series of styrylquinoline derivatives was prepared. Method: A series of styrylquinoline derivatives was prepared from quinaldic acid and a variety of arylbenzaldehydes under eco-friendly conditions via Knoevenagel reaction and trifluoroacetic acid (TFA) as catalyst. Results: The products were obtained in short reaction times and good yields and were evaluated for growth inhibitory activity towards Mycobacterium tuberculosis H37Rv (Mtb) through the National Institute of Allergy and Infectious Diseases (NIAID, USA). Conclusion: Three compounds had activity under aerobic conditions.Keywords: Synthesis, microwave, styrylquinolines, catalysis, Mycobacterium tuberculosis, tuberculosis.
Graphical Abstract
Medicinal Chemistry
Title:Microwave-assisted Synthesis of 2-Styrylquinoline-4-carboxylic Acids as Antitubercular Agents
Volume: 13 Issue: 5
Author(s): Gisela C. Muscia, Silvia E. Asis*Graciela Y. Buldain
Affiliation:
- Facultad de Farmacia y Bioquímica, Departamento de Química Orgánica, Universidad de Buenos Aires, Junín 956, C1113AAB Ciudad Autónoma de Buenos Aires,Argentina
Keywords: Synthesis, microwave, styrylquinolines, catalysis, Mycobacterium tuberculosis, tuberculosis.
Abstract: Background: Many 2-substituted quinolines and especially 2-arylvinyl derivatives isolated from plants or prepared by synthesis have been designed from ethnopharmacological studies.
Objective: In order to explore new aspects of the structure-antituberculosis activity relationship, a series of styrylquinoline derivatives was prepared. Method: A series of styrylquinoline derivatives was prepared from quinaldic acid and a variety of arylbenzaldehydes under eco-friendly conditions via Knoevenagel reaction and trifluoroacetic acid (TFA) as catalyst. Results: The products were obtained in short reaction times and good yields and were evaluated for growth inhibitory activity towards Mycobacterium tuberculosis H37Rv (Mtb) through the National Institute of Allergy and Infectious Diseases (NIAID, USA). Conclusion: Three compounds had activity under aerobic conditions.Export Options
About this article
Cite this article as:
Muscia C. Gisela, Asis E. Silvia*, Buldain Y. Graciela, Microwave-assisted Synthesis of 2-Styrylquinoline-4-carboxylic Acids as Antitubercular Agents, Medicinal Chemistry 2017; 13 (5) . https://dx.doi.org/10.2174/1573406412666160901102710
DOI https://dx.doi.org/10.2174/1573406412666160901102710 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
- 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
-
Therapeutic Drugs that Behave as Mechanism-Based Inhibitors of Cytochrome P450 3A4
Current Drug Metabolism Renaissance in Antibiotic Discovery: Some Novel Approaches for Finding Drugs to Treat Bad Bugs
Current Medicinal Chemistry Coal Mine Dust Lung Disease: The Silent Coal Mining Disaster
Current Respiratory Medicine Reviews Nitric Oxide: State of the Art in Drug Design
Current Medicinal Chemistry Recent Patents on Live Bacteria and their Products as Potential Anticancer Agents
Recent Patents on Anti-Cancer Drug Discovery Antibacterial Effects of Carbon Monoxide
Current Pharmaceutical Biotechnology Synthesis and Evaluation of Antimicrobial Activity of Thiazolidinone Derivatives
Letters in Drug Design & Discovery Biomarkers and Pneumonia: Should We All be Using Them?
Current Respiratory Medicine Reviews Virtual Screening and in vitro Antibacterial Activity for the Identification of Novel Inhibitors of Mycobacterium tuberculosis Methionine Aminopeptidase
Current Enzyme Inhibition Translation Controlled mRNAs: New Drug Targets in Infectious Diseases?
Infectious Disorders - Drug Targets Editorial
Current Drug Therapy Th2 Cytokines in Susceptibility to Tuberculosis
Current Molecular Medicine Synthesis and Evaluation of New 5-methylisoxazole-3-carboxamide Derivatives as Antitubercular Agents
Anti-Infective Agents Toll-Like Receptors and Human Disease: Lessons from Single Nucleotide Polymorphisms
Current Genomics Editorial (Thematic Issue: Polypharmacology in Drug Discovery)
Current Pharmaceutical Design Editorial: Recent Advances in the Field of Kinases and Kinase Inhibitors
Current Pharmaceutical Design Design, Synthesis and Antitubercular Evaluation of New 2-amino-5-(4- (benzyloxy)benzyl)thiophene-3-carboxylic Acid Derivatives. Part 3
Letters in Drug Design & Discovery Bacterial Proteases in Disease – Role in Intracellular Survival, Evasion of Coagulation/ Fibrinolysis Innate Defenses, Toxicoses and Viral Infections
Current Pharmaceutical Design Isoquinoline Alkaloids and Their Antiviral, Antibacterial, and Antifungal Activities and Structure-activity Relationship
Current Organic Chemistry General Aspects of Two-Component Regulatory Circuits in Bacteria: Domains, Signals and Roles
Current Protein & Peptide Science