Abstract
Synthesis, characterization and investigation of antibacterial and antifungal activities of thirteen novel 6- hydroxybenzofuran-3(2H)-one based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using NMR, FAB MS and HRMS analyses. The results of microbiological screening reveal that three derivatives containing fluorine, bromine and hydrogen substituents at the phenyl ring are the most active antimicrobial compounds. Molecular docking studies of all compounds on the active sites of microbial enzymes indicated a possible target Nmyristoyltransferase (NMT).
Keywords: Thiazoles, Thiosemicarbazones, Benzofuranone, Antimicrobial drugs, N-myristoyltransferase, Molecular modeling.
Letters in Drug Design & Discovery
Title:Synthesis, Antimicrobial Activities and Molecular Docking Studies of Novel 6-Hydroxybenzofuran-3(2H)-one Based 2,4-Disubstituted 1,3- Thiazoles
Volume: 10 Issue: 9
Author(s): Krzysztof Z. Laczkowski, Konrad Misiura, Anna Biernasiuk, Anna Malm, Agata Siwek and Tomasz Plech
Affiliation:
Keywords: Thiazoles, Thiosemicarbazones, Benzofuranone, Antimicrobial drugs, N-myristoyltransferase, Molecular modeling.
Abstract: Synthesis, characterization and investigation of antibacterial and antifungal activities of thirteen novel 6- hydroxybenzofuran-3(2H)-one based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using NMR, FAB MS and HRMS analyses. The results of microbiological screening reveal that three derivatives containing fluorine, bromine and hydrogen substituents at the phenyl ring are the most active antimicrobial compounds. Molecular docking studies of all compounds on the active sites of microbial enzymes indicated a possible target Nmyristoyltransferase (NMT).
Export Options
About this article
Cite this article as:
Laczkowski Z. Krzysztof, Misiura Konrad, Biernasiuk Anna, Malm Anna, Siwek Agata and Plech Tomasz, Synthesis, Antimicrobial Activities and Molecular Docking Studies of Novel 6-Hydroxybenzofuran-3(2H)-one Based 2,4-Disubstituted 1,3- Thiazoles, Letters in Drug Design & Discovery 2013; 10 (9) . https://dx.doi.org/10.2174/15701808113109990010
DOI https://dx.doi.org/10.2174/15701808113109990010 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Biological Activities of QIAPI 1 as a Melanin Precursor and Its Therapeutic Effects in Wistar Rats Exposed to Arsenic Poisoning
Central Nervous System Agents in Medicinal Chemistry Cationic <i>Clitoria ternatea</i> Seed Peptide as a Potential Novel Bioactive Molecule
Protein & Peptide Letters Development and Production of Commercial Therapeutic Monoclonal Antibodies in Mammalian Cell Expression Systems: An Overview of the Current Upstream Technologies
Current Pharmaceutical Biotechnology Biological Importance of Phenol Derivatives as Potent Bioactive Compound: A Review
Letters in Organic Chemistry Application of NMR Metabolomics to Search for Human Disease Biomarkers
Combinatorial Chemistry & High Throughput Screening Design, Synthesis and Biological Evaluation of 4-(Imidazolylmethyl)-2- Aryl-Quinoline Derivatives as Aromatase Inhibitors and Anti-breast Cancer Agents
Letters in Drug Design & Discovery Ginsenoside Rb1 Directly Scavenges Hydroxyl Radical and Hypochlorous Acid
Current Pharmaceutical Design Emerging Role of Cetuximab in the Treatment of Colorectal Cancer
Recent Patents on Anti-Cancer Drug Discovery A Survey of Kidney Segmentation Techniques in CT Images
Current Medical Imaging Inhibitors of the Sphingosine Kinase Pathway as Potential Therapeutics
Current Cancer Drug Targets Different Methods for Molecular and Rapid Detection of Human Novel Coronavirus
Current Pharmaceutical Design Recent Advancement in Topical Drug Delivery for Psoriasis: Clinical Pertinence and Potential Market
Current Drug Targets Fragment-Based Drug Discovery and Molecular Docking in Drug Design
Current Pharmaceutical Biotechnology Peptide Self-Assemblies for Drug Delivery
Current Topics in Medicinal Chemistry A Validated 2D-LC-UV Method for Simultaneous Determination of Imatinib and N-desmethylimatinib in Plasma and its Clinical Application for Therapeutic Drug Monitoring with GIST Patients
Current Pharmaceutical Analysis Bioinformatic Tools Identify Chromosome-Specific DNA Probes and Facilitate Risk Assessment by Detecting Aneusomies in Extra-embryonic Tissues
Current Genomics Application of Two New Feature Fusion Networks to Improve Real-time Prostate Capsula Detection
Current Medical Imaging Anticancer Activities of New N-hetaryl-2-cyanoacetamide Derivatives Incorporating 4,5,6,7-Tetrahydrobenzo[b]thiophene Moiety
Anti-Cancer Agents in Medicinal Chemistry Nanowired Drug Delivery Across the Blood-Brain Barrier in Central Nervous System Injury and Repair
CNS & Neurological Disorders - Drug Targets Physico-chemical and Biological Evaluation of Flavonols: Fisetin, Quercetin and Kaempferol Alone and Incorporated in beta Cyclodextrins
Anti-Cancer Agents in Medicinal Chemistry