Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 15, Issue 18, Pages 6291-6297Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.06.017
Keywords
2-aminobenzimidazole.; bis(benzimidazol-2-yl)amines; antitrichinellosis activity; DFT
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Novel bis(benzimidazol-2-yl)a mines 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. (c) 2007 Elsevier Ltd. All rights reserved.
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