Abstract
Antimicrobial Resistance (AMR) is a serious problem for the humans since it threatens the effective prevention and treatment of an ever-increasing range of infections caused by bacteria, parasites, viruses and fungi. One way around this problem is to act on the virulence factors, produced by bacteria, which increase their infection effectiveness. In view of these facts, new coumarin derivatives were synthesized and evaluated for their anti-virulence biological activity towards Pseudomonas aeruginosa. The results suggest that coumarin derivatives with a secondary carbon at C-3 position reduces P. aeruginosa growth whereas compounds with one additional substituent have a significant effect over pyocyanin production (10k EC50 7 ± 2 µM; 10l EC50 42 ± 13 µM). Moreover, 10k reduces P. aeruginosa motility and biofilm formation, what is compatible with a quorum sensing related mechanism of action.
Keywords: Antimicrobial resistance, anti-virulence, cellular assay, phenazine, 2H-chromen-2-one, inhibitor.
Current Topics in Medicinal Chemistry
Title:Synthesis and Biological Evaluation of Coumarins Derivatives as Potential Inhibitors of the Production of Pseudomonas aeruginosa Virulence Factor Pyocyanin
Volume: 18 Issue: 2
Author(s): Luana da S.M. Forezi, Thamires Quadros Froes, Mariana F.C. Cardoso, Carine Assuncao de Oliveira Maciel, Gianluca G. Nicastro, Regina L. Baldini, Dora C.S. Costa, Vitor F. Ferreira, Marcelo S. Castilho*Fernando de C. da Silva*
Affiliation:
- Departamento de Quimica Organica, Universidade Federal Fluminense, Instituto de Quimica, Niteroi, RJ, 24020-150,Brazil
- Departamento de Quimica Organica, Universidade Federal Fluminense, Instituto de Quimica, Niteroi, RJ, 24020-150,Brazil
Keywords: Antimicrobial resistance, anti-virulence, cellular assay, phenazine, 2H-chromen-2-one, inhibitor.
Abstract: Antimicrobial Resistance (AMR) is a serious problem for the humans since it threatens the effective prevention and treatment of an ever-increasing range of infections caused by bacteria, parasites, viruses and fungi. One way around this problem is to act on the virulence factors, produced by bacteria, which increase their infection effectiveness. In view of these facts, new coumarin derivatives were synthesized and evaluated for their anti-virulence biological activity towards Pseudomonas aeruginosa. The results suggest that coumarin derivatives with a secondary carbon at C-3 position reduces P. aeruginosa growth whereas compounds with one additional substituent have a significant effect over pyocyanin production (10k EC50 7 ± 2 µM; 10l EC50 42 ± 13 µM). Moreover, 10k reduces P. aeruginosa motility and biofilm formation, what is compatible with a quorum sensing related mechanism of action.
Export Options
About this article
Cite this article as:
da S.M. Forezi Luana , Froes Quadros Thamires , Cardoso F.C. Mariana , de Oliveira Maciel Assuncao Carine , Nicastro G. Gianluca , Baldini L. Regina , Costa C.S. Dora , Ferreira F. Vitor , Castilho S. Marcelo *, de C. da Silva Fernando *, Synthesis and Biological Evaluation of Coumarins Derivatives as Potential Inhibitors of the Production of Pseudomonas aeruginosa Virulence Factor Pyocyanin, Current Topics in Medicinal Chemistry 2018; 18 (2) . https://dx.doi.org/10.2174/1568026618666180329122704
DOI https://dx.doi.org/10.2174/1568026618666180329122704 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...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
- Announcements
Related Articles
-
Enhanced Hippocampal Neurogenesis in APP/Ps1 Mouse Model of Alzheimer's Disease After Implantation of VEGF-loaded PLGA Nanospheres
Current Alzheimer Research Depression and Vascular Disease: Conceptual Issues, Relationships and Clinical Implications
Vascular Disease Prevention (Discontinued) Interleukin-1β Increases Release of Endothelin-1 and Tumor Necrosis Factor as Well as Reactive Oxygen Species by Peripheral Leukocytes During Experimental Subarachnoid Hemorrhage
Current Neurovascular Research Manganese Superoxide Dismutase (Sod2) and Redox-Control of Signaling Events That Drive Metastasis
Anti-Cancer Agents in Medicinal Chemistry Crosstalk Between the Angiotensin and Endothelin-System in the Cerebrovasculature
Current Neurovascular Research Carbonic Anhydrase Activation and the Drug Design
Current Pharmaceutical Design Marrow Stromal Cells: Implications in Health and Disease in the Nervous System
Current Molecular Medicine Inhibition of Pancreatic Ribonuclease A Aggregation by Antibodies Raised Against the Native Enzyme and Its N-Terminal Dodecapeptide
Protein & Peptide Letters MYC-mediated Synthetic Lethality for Treatment of Hematological Malignancies
Current Cancer Drug Targets Sympathetic Signaling in Angiogenesis: Implications for Cancer Progression
Current Cancer Therapy Reviews Development of Validated Stability Indicating HPTLC Method for the Estimation of Teriflunomide in Bulk and Tablet Dosage Form
Current Pharmaceutical Analysis Clinical Applications for Cardiovascular Magnetic Resonance Imaging at 3 Tesla
Current Cardiology Reviews Melatonin and Renal Protection: Novel Perspectives from Animal Experiments and Human Studies (Review)
Current Pharmaceutical Design Noradrenergic Regulation of Hippocampus-Dependent Memory
Central Nervous System Agents in Medicinal Chemistry Scopolamine and Depression: A Role for Muscarinic Antagonism?
CNS & Neurological Disorders - Drug Targets The Therapeutic Potential of Sigma (σ) Receptors for the Treatment of Central Nervous System Diseases: Evaluation of the Evidence
Current Pharmaceutical Design Molecular Docking Studies of Flavonoids Derivatives on the Flavonoid 3- O-Glucosyltransferase
Current Computer-Aided Drug Design Transcranial Direct Current Stimulation for the Treatment of Refractory Symptoms of Schizophrenia. Current Evidence and Future Directions
Current Pharmaceutical Design Justification for Domestic Violence and Women’s Autonomy in Zambia
Applied Clinical Research, Clinical Trials and Regulatory Affairs Influence of CYP2D6 Genetics on Opioid Kinetics, Metabolism and Response
Current Pharmacogenomics