Synthesis and antitrichinellosis activity of some bis(benzimidazol-2-yl)amines

详细信息	查看全文 | 推荐本文 |

• 作者：Anelia Ts. Mavrova ; Pavletta Denkova ; Yordan A. Tsenov ; Kameliya K. Anichina ; Dimitar I. Vutchev
• 关键词：2-Aminobenzimidazole ; Bis(benzimidazol-2-yl)amines ; Antitrichinellosis activity ; DFT
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2007
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 September 2007
• 卷：15
• 期：18
• 页码：6291-6297
• 文件大小：165 K

摘要

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 100 mg/kg mw, while albendazole possesses 100%efficacy only at a dose of 100 mg/kg mw.