Mavrova Anelia Ts, Denkova Pavletta, Tsenov Yordan A, Anichina Kameliya K, Vutchev Dimitar I
Department of Organic Synthesis, University of Chemical Technology and Metallurgy, 8 Kliment Ohridski Blvd., 1756 Sofia, Bulgaria.
Bioorg Med Chem. 2007 Sep 15;15(18):6291-7. doi: 10.1016/j.bmc.2007.06.017. Epub 2007 Jun 13.
Novel bis(benzimidazol-2-yl)amines were synthesized using two methods and studied for antitrichinellosis activity. DFT calculations were performed in order to determine the geometry of molecules. All derivatives of 2-aminobenzimidazole exhibited higher activity in vitro against Trichinella spiralis larvae in regard to the activity of albendazole, moreover compounds 4f-i manifested antitrichinellosis effect, which surpassed five times the activity of albendazole. The in vivo screening of intestinal phase of the T. spiralis revealed 100% effectiveness of compounds 4g-i at oral dosages of 50 and 100mg/kgmw, while albendazole possesses 100% efficacy only at a dose of 100mg/kgmw.
采用两种方法合成了新型双（苯并咪唑-2-基）胺，并对其抗旋毛虫活性进行了研究。进行了密度泛函理论（DFT）计算以确定分子的几何结构。就阿苯达唑的活性而言，2-氨基苯并咪唑的所有衍生物在体外对旋毛虫幼虫均表现出更高的活性，此外，化合物4f-i表现出抗旋毛虫病的效果，其活性超过阿苯达唑的五倍。旋毛虫肠道期的体内筛选显示，化合物4g-i在口服剂量为50和100mg/kg体重时具有100%的有效性，而阿苯达唑仅在剂量为100mg/kg体重时具有100%的疗效。
