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 100mg/kgmw, while albendazole possesses 100% efficacy only at a dose of 100mg/kgmw.
Mavrova
Anelia Ts
ATs
Department of Organic Synthesis, University of Chemical Technology and Metallurgy, 8 Kliment Ohridski Blvd., 1756 Sofia, Bulgaria. anmav@abv.bg
Denkova
Pavletta
P
Tsenov
Yordan A
YA
Anichina
Kameliya K
KK
Vutchev
Dimitar I
DI
D000588:Amines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D007411:Intestinal Diseases, Parasitic / Q000188:drug therapy; D007814:Larva / Q000187:drug effects*; D051379:Mice; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D017160:Trichinella spiralis / Q000187:drug effects* / Q000254:growth & development; D014235:Trichinellosis / Q000188:drug therapy* / Q000378:metabolism / Q000517:prevention & control
D000588:Amines; D000871:Anthelmintics; D001562:Benzimidazoles