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

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.

New derivatives of 2-aminobenzimidazole were synthesized using two methods and studied for antitrichinellosis activity. The in vitro and in vivo screening of the intestinal phase of Trichinella spiralis exhibited significant effectiveness of the investigated compounds.Figure optionsDownload as PowerPoint slide