Abstract
Background: A series of new 6-(tert-butyl)-8-chloro-2,3-dimethyl quinoline derivatives were designed and synthesized.
Results: The primarily antifungal assay results indicated that all of them exhibited excellent protective efficacy (100%) against Pyricularia oryae at 100 ppm, except compound 2m (90%). Among them, the compound 2p (6-(tert-butyl)-8-chloro-2,3-dimethylquinolin-4-yl(2-chloro-5- (trifluoromethyl)benzyl)carbonate) possessed the highest fungicidal efficacy against Pyricularia oryae, even at 10 ppm.
Conclusion: The structure-activity relationship showed that when the 2-position of benzene ring was substituted by F or Cl, the compound possessed good antifungal activity against Pyricularia oryae.
Keywords: Quinoline, antifungal activity, SAR, benzene, Pyricularia oryae, heterocyclic compounds.
Letters in Drug Design & Discovery
Title:Synthesis and Antifungal Activity of Some 6-tert-butyl-8-chloro-2, 3-dimethylquinolin-4-ol Derivatives against Pyricularia oryae
Volume: 15 Issue: 12
Author(s): Yue-Ming Fang, Rui-Rui Zhang, Zhong-Hua Shen, Cheng-Xia Tan, Jian-Quan Weng, Tian-Ming Xu*, Xing-Hai Liu*, Hong-Ying Huang and Hong-Ke Wu
Affiliation:
- Zhejiang Base of National Southern Pesticide Research Centre, Zhejiang Research Institute of Chemical Industry, Hangzhou 310023,China
- College of Chemical Engineering, Zhejiang University of Technology, Hangzhou, 310014,China
Keywords: Quinoline, antifungal activity, SAR, benzene, Pyricularia oryae, heterocyclic compounds.
Abstract: Background: A series of new 6-(tert-butyl)-8-chloro-2,3-dimethyl quinoline derivatives were designed and synthesized.
Results: The primarily antifungal assay results indicated that all of them exhibited excellent protective efficacy (100%) against Pyricularia oryae at 100 ppm, except compound 2m (90%). Among them, the compound 2p (6-(tert-butyl)-8-chloro-2,3-dimethylquinolin-4-yl(2-chloro-5- (trifluoromethyl)benzyl)carbonate) possessed the highest fungicidal efficacy against Pyricularia oryae, even at 10 ppm.
Conclusion: The structure-activity relationship showed that when the 2-position of benzene ring was substituted by F or Cl, the compound possessed good antifungal activity against Pyricularia oryae.
Export Options
About this article
Cite this article as:
Fang Yue-Ming, Zhang Rui-Rui , Shen Zhong-Hua, Tan Cheng-Xia, Weng Jian-Quan, Xu Tian-Ming *, Liu Xing-Hai*, Huang Hong-Ying and Wu Hong-Ke, Synthesis and Antifungal Activity of Some 6-tert-butyl-8-chloro-2, 3-dimethylquinolin-4-ol Derivatives against Pyricularia oryae, Letters in Drug Design & Discovery 2018; 15 (12) . https://dx.doi.org/10.2174/1570180815666180313121735
DOI https://dx.doi.org/10.2174/1570180815666180313121735 |
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
-
Microbial Biodiscovery: Back to the Future
Current Topics in Medicinal Chemistry Inhibitors of the Sulfur Assimilation Pathway in Bacterial Pathogens as Enhancers of Antibiotic Therapy
Current Medicinal Chemistry A Network Science-Based Performance Improvement Model for the Airline Industry Using NetworkX
International Journal of Sensors, Wireless Communications and Control Therapeutic Potential of Adipose-derived Stem Cells in the Treatment of Pulmonary Diseases
Current Stem Cell Research & Therapy Novel Hybrid Anticonvulsants Derived from Pyrrolidine-2,5-dione Scaffold with Broad Spectrum of Activity in the Preclinical Studies
Current Topics in Medicinal Chemistry Natural Compounds as Heme Oxygenase-1 Inducers to Reduce the Deleterious Consequences Following SARS-CoV-2 Infection
Current Chemical Biology Repurposing Drugs for the Management of Patients with Confirmed Coronavirus Disease 2019 (COVID-19)
Current Pharmaceutical Design Cyclosporin A: A Therapeutic Strategy in Allergic Diseases
Letters in Drug Design & Discovery Integration of Virtual and High Throughput Screening in Lead Discovery Settings
Combinatorial Chemistry & High Throughput Screening Factors Influencing Outcome of Patients Receiving Extracorporeal Membrane Oxygenation for Neonatal and Pediatric Respiratory Failure
Current Respiratory Medicine Reviews Therapeutic Potential of Naturally Occurring Benzofuran Derivatives and Hybrids of Benzofurans with other Pharmacophores as Antibacterial Agents
Current Topics in Medicinal Chemistry Lipophilicity and Other Parameters Affecting Brain Penetration
Current Medicinal Chemistry - Central Nervous System Agents Synthesis of Metronidazole Derivatives Containing Pyridine Ring and Anticancer Activity
Letters in Organic Chemistry Proteasome Inhibitors: Recent Advances and New Perspectives In Medicinal Chemistry
Current Topics in Medicinal Chemistry Nephrotic Syndrome and Renin-angiotensin System: Pathophysiological Role and Therapeutic Potential
Current Molecular Pharmacology Generating a Biological Pacemaker - Tackling Arrhythmias the Stem Cell Way
Recent Patents on Regenerative Medicine Adenosine Receptor Ligands-Recent Developments Part I. Agonists
Current Medicinal Chemistry Development of Aminoglycoside Antibiotics by Carbohydrate Chemistry
Mini-Reviews in Medicinal Chemistry Exit from Mycobacterial Dormancy: A Structural Perspective
Current Medicinal Chemistry Targeting Lipoxygenases (LOs): Drug Design And Discovery
Current Enzyme Inhibition