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

被引:95
作者
Rossiter, S
Péron, JM
Whitfield, PJ
Jones, K
机构
[1] Kings Coll London, Dept Chem, London WC2R 2LS, England
[2] Kingston Univ, Sch Chem & Pharmaceut Sci, Kingston upon Thames KT1 2EE, Surrey, England
[3] Kings Coll London, Div Life Sci, London SE1 9NN, England
基金
英国惠康基金;
关键词
quinolines; Suzuki coupling; anthelmintics;
D O I
10.1016/j.bmcl.2005.07.044
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4806 / 4808
页数:3
相关论文
共 10 条
  • [1] Albonico M, 2003, B WORLD HEALTH ORGAN, V81, P343
  • [2] Anthelmintic resistance in sheep nematodes in Australia: the need for new approaches
    Besier, RB
    Love, SCJ
    [J]. AUSTRALIAN JOURNAL OF EXPERIMENTAL AGRICULTURE, 2003, 43 (12) : 1383 - 1391
  • [3] Demethylation of 2,4-dimethoxyquinolines: the synthesis of atanine
    Jones, K
    Roset, X
    Rossiter, S
    Whitfield, P
    [J]. ORGANIC & BIOMOLECULAR CHEMISTRY, 2003, 1 (24) : 4380 - 4383
  • [4] LACEY E, RESISTANCE PARASITES, P177
  • [5] PALLADIUM-CATALYZED CROSS-COUPLING REACTIONS OF ORGANOBORON COMPOUNDS
    MIYAURA, N
    SUZUKI, A
    [J]. CHEMICAL REVIEWS, 1995, 95 (07) : 2457 - 2483
  • [6] ATANINE (3-DIMETHYLALLYL-4-METHOXY-2-QUINOLONE), AN ALKALOID WITH ANTHELMINTIC ACTIVITY FROM THE CHINESE MEDICINAL PLANT, EVODIA-RUTAECARPA
    PERRETT, S
    WHITFIELD, PJ
    [J]. PLANTA MEDICA, 1995, 61 (03) : 276 - 278
  • [7] ROSSITER S, 1999, THESIS U LONDON
  • [8] STAVENUIER J, 1987, HETEROCYCLES, V10, P2711
  • [9] Resistance of gastrointestinal nematodes to anthelmintics in sheep (Ovis aries)
    Thomaz-Soccol, V
    de Souza, FP
    Sotomaior, C
    Castro, EA
    Milczewski, V
    Mocelin, G
    Silva, MDCPE
    [J]. BRAZILIAN ARCHIVES OF BIOLOGY AND TECHNOLOGY, 2004, 47 (01) : 41 - 47
  • [10] Ziegler E., 1959, MONATSH CHEM, V90, P822