Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes.
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 LD99 values of the same order of magnitude as levamisole. These arylquinolines maintain their activity against levamisole-, ivermectin- and thiabendazole-resistant strains of H. contortus.
Rossiter
Sharon
S
Department of Chemistry, King's College London, Strand, London WC2R 2LS, UK.
Péron
Jean-Marie
JM
Whitfield
Philip J
PJ
Jones
Keith
K
D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000494:pharmacology; D000969:Antinematodal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D004351:Drug Resistance; D006188:Haemonchiasis / Q000188:drug therapy / Q000662:veterinary; D009348:Nematoda / Q000187:drug effects*; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D012756:Sheep / Q000469:parasitology; D013329:Structure-Activity Relationship
D000871:Anthelmintics; D000969:Antinematodal Agents; D011804:Quinolines