CAS: 90509-02-7; Luxabendazole

该化合物是兽医学中的化学剂;它属于联苯胺甲醇类化合物,其特点是对寄生虫的广泛频谱活动;Luxabendazole展示了一种行动机制,它涉及抑制寄生虫中微囊形成,导致其固定和最终死亡;该化合物的施用方式通常是一种能提高其生物利用率和功效的配方;就物理特性而言,Luxabendazole一般是白到白的晶状固体,有机溶剂中含有中等溶性,水溶性有限;在各种环境条件下,它的稳定使其适于用于制药制剂;安全性和毒性特征是其应用中的基本考虑因素,并且需要进行监管评估,以确保其在目标动物物种中的安全使用;

结构式图片

上下游产品

5-羟基-2-苯并咪唑氨基甲酸甲酯 (5-Hydroxy-1(3)H-Benzoimidazol-2-yl)-Carbamic Acid Methyl Ester 22769-68-2

合成工艺路线路线简述

    1,2-Diamino-4-(4-Fluorophenylsulfonyloxy)Benzene,1,3-二羧甲基-2-甲基-2-硫代异脲 反应生成 5-羟基-2-苯并咪唑氨基甲酸甲酯对氟苯磺酰酯
    参考文献:Roesner,M.;Loewe,H.;Duewel,D.;Kirsch,R.
    标题:Roesner,M.;Loewe,H.;Duewel,D.;Kirsch,R.

    海关参考信息

    专利信息


    专利号:US-7893271-B2
    优先权日:2005-07-28
    标 题 :Benzimidazole carbamates and (thio) carbamates, and the synthesis and use thereof
    发明人:CHASSAING CHRISTOPHE PIERRE ALAIN
    权利人:INTERVET INT BV
    摘要:This invention relates to benzimidazole carbamates and (thio)carbamates corresponding to Formula I: n nHere, X 1 and X 2 are independently O or S, wherein at least one of X 1 and X 2 is O; Y 1 and Y 2 are independently O or S, wherein at least one of Y 1 and Y 2 is O; R 1 is alkyl having from 1-4 carbon atoms; R 2 , R 3 , and R 4 are independently hydrogen or a cation; R 5 and R 6 are independently hydrogen, halogen, alkyl (having from 1-8 carbon atoms), —OR 7 , —SR 8 , —CO—R 9 , —OSO 2 —Ar, or —S(O)R 10 ; R 7 is alkyl having from 1-8 carbon atoms; R 8 is alkyl (having from 1-8 carbon atoms) or aryl; R 9 is alkyl (having from 1-8 carbon atoms), cycloalkyl (having from 3-6 carbon atoms), or aryl; Ar is aryl; and R 10 is alkyl (having from 1-8 carbon atoms) or aryl. The compounds generally are soluble and stable in water, and have antiparasitic (particularly anthelmintic) activity in vivo that is comparable to known water-insoluble benzimidazole carbamates (e.g., albendazole and fenbendazole).

    专利号:ES-2344275-T3
    优先权日:2005-07-28
    标 题 :NEW (UNCLE) CARBAMATES FROM BENZIMIDAZOL WITH ANTIPARASITARY ACTIVITY AND SYNTHESIS OF THEM.

    专利号:PT-1913009-E
    优先权日:2005-07-28
    标 题 :NEW (TIO) CARBAMATES OF BENZIMIDAZOLE WITH ANTIPARASITARY ACTIVITY AND ITS SYNTHESIS
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    主要参考文献


    1: Criado-Fornelio A, de Armas-Serra C, Jimenez-Gonzalez A, Casado-Escribano N, Rodriguez-Caabeiro F. Biochemical effects of luxabendazole on Trichinella spiralis. Parasitol Res. 1990;76(6):518-20.

    合成参考文献


    参考文献:10.1007/bf00931507
    摘要:Pérez-Serrano J, Denegri G, Casado N, Bodega G, Rodríguez-Caabeiro F. Anti-tubulin immunohistochemistry study of Echinococcus granulosus protoscolices incubated with albendazole and albendazole sulphoxide in vitro. Parasitol Res. 1995;81(5):438–40. doi: 10.1007/bf00931507.
    参考文献:10.1017/s0022149x00013511
    摘要:Stoitsova SR, Gorchilova LN. Effects of luxabendazole on the tegument of Fasciola hepatica. J Helminthol. 1994 Mar;68(1):73–80. doi: 10.1017/s0022149x00013511.
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