新型合成驱虫化合物——氨基乙腈衍生物的发现。
Discovery of amino-acetonitrile derivatives, a new class of synthetic anthelmintic compounds.
作者信息
Ducray Pierre, Gauvry Noëlle, Pautrat François, Goebel Thomas, Fruechtel Joerg, Desaules Yves, Weber Sandra Schorderet, Bouvier Jacques, Wagner Trixie, Froelich Olivier, Kaminsky Ronald
机构信息
Novartis Animal Health Inc., Chemistry and Bioactives, Schwarzwaldallee 215, CH-4002 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2008 May 1;18(9):2935-8. doi: 10.1016/j.bmcl.2008.03.071. Epub 2008 Mar 29.
A new series of amino-acetonitrile derivatives (AAD) have been discovered that exhibit high anthelmintic activity against parasitic nematode species such as Haemonchus contortus and Trichostrongylus colubriformis. Significantly, these compounds also demonstrate activity against nematode strains resistant to the currently available broad-spectrum anthelmintics. The discovery, synthesis, structure-activity relationship and biological results are presented.
已发现一系列新型氨基乙腈衍生物（AAD），它们对捻转血矛线虫和蛇形毛圆线虫等寄生线虫物种具有高驱虫活性。重要的是，这些化合物对目前可用的广谱驱虫药耐药的线虫菌株也有活性。本文介绍了其发现、合成、构效关系及生物学结果。
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