5-（4-水杨酰基-哌嗪-1-基）-苯并咪唑-2-氨基甲酸甲酯的合成及其潜在驱虫活性
Synthesis and potential anthelmintic activity of methyl-5-(4-salicyloyl-piperazin-1-yl)-benzimidazole-2-carbamates.
作者信息
Ravina E, Sanchez-Alonso R, Fueyo J, Baltar M P, Bos J, Iglesias R, Sanmartin M L
机构信息
Department of Organic Chemistry, Laboratory of Pharmaceutical Chemistry, University of Santiago de Compostela, Spain.
出版信息
Arzneimittelforschung. 1993 Jun;43(6):689-94.
A series of methyl-5-(4-salicyloyl-piperazin-1-yl)-benzimidazole-2-carba mates (IX) has been prepared. 5-(4-Salicyloyl-piperazin-1-yl)-2-nitro anilines (VII) have been synthesized starting from 5-piperazino-2-nitro anilines and salicyloyl chlorides. Catalytic reduction of VII with Pd/C, followed by treatment with 1,3-dicarbomethoxy-S-methyl isothiourea, yielded the corresponding carbamates (IX), the anthelmintic activity of which was studied. Compound IXa significantly reduced the numbers of preadults, adults and encysted T. spiralis larvae in experimental mice.
已制备出一系列5-（4-水杨酰基-哌嗪-1-基）-甲基苯并咪唑-2-羧酸酯（IX）。5-（4-水杨酰基-哌嗪-1-基）-2-硝基苯胺（VII）由5-哌嗪基-2-硝基苯胺和水杨酰氯合成。VII用钯/碳催化还原，然后用1,3-二羧甲基-S-甲基异硫脲处理，得到相应的羧酸酯（IX），并对其驱虫活性进行了研究。化合物IXa显著减少了实验小鼠体内旋毛虫未成熟虫体、成虫和包囊幼虫的数量。
Zotero 插件