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  • Title: Synthesis and antitrichinellosis activity of some bis(benzimidazol-2-yl)amines.
    Author: Mavrova ATs, Denkova P, Tsenov YA, Anichina KK, Vutchev DI.
    Journal: Bioorg Med Chem; 2007 Sep 15; 15(18):6291-7. PubMed ID: 17600722.
    Abstract:
    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.
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