KMID : 0043320130360121465
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Archives of Pharmacal Research 2013 Volume.36 No. 12 p.1465 ~ p.1479
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Design, synthesis and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetohydrazide derivatives with anti-inflammatory-analgesic activities
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Mohammed Anber F.
Abdel Moty Samia G. Hussein Mostafa A. Abdel Alim Abdel Alim M.
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Abstract
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The present work describes the synthesis and evaluation of some new acetohydrazones, 1,3,4-oxadiazoles and 1,2,4-triazoles of 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflamm atory-analgesic agents. Structure elucidation of these compounds was confirmed by IR, 1H NMR, and mass spectrometry along with elemental microanalyses. Most compounds exhibited significant anti-inflammatory activity in comparison to indomethacin. Further, some compounds were tested for their analgesic effects where two compounds showed 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¡¯t show any gastric ulcerogenic effect compared with the reference indomethacin. Moreover, LD50 of compounds (4c and 11a) were determined in mice; they were found non toxic up to 240 and 300 mg/kg (i.p.). Also, docking simulation of some compounds into COX active sites was studied.
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KEYWORD
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1,2,4-Triazolobenzimidazole, Anti-inflammatory-analgesic, Ulcerogenecity, COX enzyme, Molecular docking
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