Abstract
The dramatic worldwide increase of dangerous infections by resistant and multi-resistant microbes makes the search of new molecules and new chemical entities an important topic in Medicinal Chemistry. As the ideal drug candidate has not been attained, an intensive search for new and innovative antimicrobials is still needed. A small series of 3- amino/nitrocoumarins without substitutions or substituted by methyl or methoxy groups at different positions were synthesized and evaluated for their antibacterial and antifungal activities against clinical isolates of Staphylococcus aureus, Escherichia coli and Candida albicans strains. Some of these structurally simple molecules exhibited antibacterial activity. The preliminary SAR study showed that the antibacterial activity against E. coli and S. aureus was dependent on the kind and position of the substitution pattern at the coumarin moiety.
Keywords: Aminocoumarins, nitrocoumarins, coumarin synthesis, antibacterial assays, inhibition zones, minimum inhibitory concentrations, S. aureus, E. coli
Medicinal Chemistry
Title:Looking for New Targets: Simple Coumarins as Antibacterial Agents
Volume: 8 Issue: 6
Author(s): Maria Joao Matos, Saleta Vazquez-Rodriguez, Lourdes Santana, Eugenio Uriarte, Cristina Fuentes-Edfuf, Ysabel Santos and Angeles Munoz-Crego
Affiliation:
Keywords: Aminocoumarins, nitrocoumarins, coumarin synthesis, antibacterial assays, inhibition zones, minimum inhibitory concentrations, S. aureus, E. coli
Abstract: The dramatic worldwide increase of dangerous infections by resistant and multi-resistant microbes makes the search of new molecules and new chemical entities an important topic in Medicinal Chemistry. As the ideal drug candidate has not been attained, an intensive search for new and innovative antimicrobials is still needed. A small series of 3- amino/nitrocoumarins without substitutions or substituted by methyl or methoxy groups at different positions were synthesized and evaluated for their antibacterial and antifungal activities against clinical isolates of Staphylococcus aureus, Escherichia coli and Candida albicans strains. Some of these structurally simple molecules exhibited antibacterial activity. The preliminary SAR study showed that the antibacterial activity against E. coli and S. aureus was dependent on the kind and position of the substitution pattern at the coumarin moiety.
Export Options
About this article
Cite this article as:
Joao Matos Maria, Vazquez-Rodriguez Saleta, Santana Lourdes, Uriarte Eugenio, Fuentes-Edfuf Cristina, Santos Ysabel and Munoz-Crego Angeles, Looking for New Targets: Simple Coumarins as Antibacterial Agents, Medicinal Chemistry 2012; 8 (6) . https://dx.doi.org/10.2174/1573406411208061140
DOI https://dx.doi.org/10.2174/1573406411208061140 |
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
-
Synthesis and Cytotoxicity of Enediyne Prodrugs with 3-Hydroxy-4- (arylmethylidene)cyclodeca-1,5-diyne Scaffolds
Letters in Drug Design & Discovery A Review on Structure-Activity Relationships of Glycyrrhetinic Acid Derivatives with Diverse Bioactivities
Mini-Reviews in Medicinal Chemistry Role of Ca2+-Sensitive K+ Currents in Controlling Ventricular Repolarization: Possible Implications for Future Antiarrhytmic Drug Therapy
Current Medicinal Chemistry PET and SPECT Imaging in the SARS-CoV-2 Pandemic
Current Radiopharmaceuticals Caspase Inhibitors: A Pharmaceutical Industry Perspective
Current Topics in Medicinal Chemistry Doripenem: A New Addition to the Carbapenem Class of Antimicrobials
Recent Patents on Anti-Infective Drug Discovery Synthetic Glycosides and Glycoconjugates of Low Molecular Weight Natural Products
Current Pharmaceutical Design Dual-acting of Hybrid Compounds - A New Dawn in the Discovery of Multi-target Drugs: Lead Generation Approaches
Current Topics in Medicinal Chemistry Matrix Metalloproteinase Inhibitors as Prospective Agents for the Prevention and Treatment of Cardiovascular and Neoplastic Diseases
Current Topics in Medicinal Chemistry Systemic and Biophase Bioavailability and Pharmacokinetics of Nanoparticulate Drug Delivery Systems
Current Drug Delivery Exploring the Targets of Novel Corona Virus and Docking-based Screening of Potential Natural Inhibitors to Combat COVID-19
Current Topics in Medicinal Chemistry Anti-MRSA Cephems: An Update
Current Medicinal Chemistry - Anti-Infective Agents COVID-19 in Patients with Systemic Inflammatory Diseases: Impact on Disease Activity
Current Rheumatology Reviews Clinical Pharmacology of Theophylline in Preterm Infants: Effects, Metabolism and Pharmacokinetics
Current Pediatric Reviews Oxidative Stress and Antioxidant Potential of One Hundred Medicinal Plants
Current Topics in Medicinal Chemistry From Multiple PAR1 Receptor/Protein Interactions to their Multiple Therapeutic Implications
Current Topics in Medicinal Chemistry Molecular Modeling Studies of Novel Fluoroquinolone Molecules
Current Drug Discovery Technologies Novel Therapeutic Potential of Mitogen-Activated Protein Kinase Activated Protein Kinase 2 (MK2) in Chronic Airway Inflammatory Disorders
Current Drug Targets A New Multicomponent Reaction MCR4 for the Synthesis of Analogs of Staurosporine
Current Organic Chemistry Immediate and Late Adverse Reactions to Iodinated Contrast Media: A Pharmacological Point of View
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry