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Anber F. Mohammed,Samia G. Abdel-Moty,Mostafa A. Hussein,Abdel Alim M. Abdel Alim 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.12
The present work describes the synthesis andevaluation of some new acetohydrazones, 1,3,4-oxadiazolesand 1,2,4-triazoles of 1,2,4-triazolo[1,5-a]benzimidazole asanti-inflamm atory-analgesic agents. Structure elucidation ofthese compounds was confirmed by IR, 1H NMR, and massspectrometry along with elemental microanalyses. Mostcompounds exhibited significant anti-inflammatory activityin comparison to indomethacin. Further, some compoundswere tested for their analgesic effects where two compoundsshowed results comparable to indomethacin at 4 h interval. The most active anti-inflammatory and analgesic compounds(4c and 11a) were examined on gastric mucosa and didn’tshow any gastric ulcerogenic effect compared with the referenceindomethacin. Moreover, LD50 of compounds (4c and11a) were determined in mice; they were found non toxic upto 240 and 300 mg/kg (i.p.). Also, docking simulation ofsome compounds into COX active sites was studied.