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
-
Variation of pKa in the N-Terminal Tyrosine Side Chain in Octapeptide Analogs of Tendamistat Influences α-Amylase Inhibition
Protein & Peptide Letters NPY Y1 and Y5 Receptor Selective Antagonists as Anti-Obesity Drugs
Current Topics in Medicinal Chemistry Recent Patents in Antiviral siRNAs
Recent Patents on Anti-Infective Drug Discovery Preface
Recent Advances in Drug Delivery and Formulation Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents
Letters in Drug Design & Discovery Synthesis and Evaluation of Amido-Deoxyestradiol Derivatives as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 12
Current Enzyme Inhibition Synthetic Glycosides and Glycoconjugates of Low Molecular Weight Natural Products
Current Pharmaceutical Design From Polypharmacology to Target Specificity: The Case of PARP Inhibitors
Current Topics in Medicinal Chemistry Mini-Review on SARS-CoV-2 Infection and Neurological Manifestations: A Perspective
CNS & Neurological Disorders - Drug Targets Current Trends in Virtual High Throughput Screening Using Ligand-Based and Structure-Based Methods
Combinatorial Chemistry & High Throughput Screening Withdrawal Notice: In Drug Repurposing Tactics against Covid-19
Current Psychopharmacology Inflammation and Chronic Heart Failure: From Biomarkers to Novel Anti-inflammatory Therapeutic Strategies
Medicinal Chemistry Phosphodiesterase 5 Inhibitors - Drug Design and Differentiation Based on Selectivity, Pharmacokinetic and Efficacy Profiles
Current Pharmaceutical Design Withdrawal Notice: Emerging Novel Coronavirus is a Global Threat: Insight in the Biology of COVID-19 and its Hijacking Process of Hosts’ Cell
Current Pharmaceutical Design Impacts and Consequences of COVID-19 Epidemic on Global Economy
Coronaviruses Computational Approaches on Angiotensin Receptors and Their Ligands: Recent Developments and Results
Current Medicinal Chemistry Mixed Lineage Kinase Family, Potential Targets for Preventing Neurodegeneration
Current Medicinal Chemistry - Central Nervous System Agents Coronavirus in the Arena: One More Time
Current Respiratory Medicine Reviews Food Allergy
Current Pharmaceutical Design Transdermal Anti-inflammatory Delivery for Solid Lipid Nanoparticles of Ketoprofen by Microwave-assisted Microemulsion
Recent Advances in Inflammation & Allergy Drug Discovery