Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes

A number of aryl-substituted 2,4-dimethoxyquinolines have been synthesized and tested against a range of nematodes. The 6-substituted compounds show significant activity against resistant strains. 2,4-Disubstituted quinolines with additional substituents in positions 5–8 have been found to have anth...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 15; no. 21; pp. 4806 - 4808
Main Authors Rossiter, Sharon, Péron, Jean-Marie, Whitfield, Philip J., Jones, Keith
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 01.11.2005
Elsevier
Subjects
Animals
Anthelmintics
Anthelmintics - chemical synthesis
Anthelmintics - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antinematodal Agents - chemical synthesis
Antinematodal Agents - pharmacology
Antiparasitic agents
Biological and medical sciences
Drug Resistance
Haemonchiasis - drug therapy
Haemonchiasis - veterinary
Medical sciences
Nematoda - drug effects
Pharmacology. Drug treatments
Quinolines
Quinolines - chemical synthesis
Quinolines - pharmacology
Sheep - parasitology
Structure-Activity Relationship
Suzuki coupling
Quinolines
Suzuki coupling
Anthelmintics
Haemonchus contortus
Tiabendazole drug
Anthelmintic
Nitrogen heterocycle
Veterinary medicine
Structure activity relation
Bicyclic compound
Aromatic compound
Chemical synthesis
Nematoda
Drug
Ether
Benzene derivatives
Levamisole
Quinoline derivatives
In vitro
Resistance
Helmintha
Parasiticide
Nemathelminthia
Invertebrata
Ivermectin
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Summary:A number of aryl-substituted 2,4-dimethoxyquinolines have been synthesized and tested against a range of nematodes. The 6-substituted compounds show significant activity against resistant strains. 2,4-Disubstituted quinolines with additional substituents in positions 5–8 have been found to have anthelmintic properties. A number of 2,4-dimethoxy-6- or 8-arylquinolines have potent activity against the sheep nematode Haemonchus contortus, with LD 99 values of the same order of magnitude as levamisole. These arylquinolines maintain their activity against levamisole-, ivermectin- and thiabendazole-resistant strains of H. contortus.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.07.044