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Synthesis, Biological Evaluation and Molecular Modeling Study of Substituted 1,2,4-Triazole-3-Acetic Acid Derivatives

مؤلف البحث
Hend A. A. Abd El-Wahab, Hamdy M. Abdel-Rahman, Gamal-Eldin S. Alkaramany, Mahmoud A. El-Gendy
مجلة البحث
Der Pharma Chemica,
تصنيف البحث
1
عدد البحث
Vol.3, No.6
سنة البحث
2011
المشارك في البحث
ملخص البحث

A series of 1,2,4-triazole-3-acetamides 3a-b, 1-acylated-1,2,4-triazole-3- acetamides 4a-b, ethyl 5-(2-substitutedacetamido)-1H-1,2,4-triazole-3-acetates 6, 7, 8, ethyl 1- substituted (carbamoyl and thiocarbamoyl)-5-amino-1H-1,2,4-triazole-3-acetates 9a-j and ethyl 5-(3(4-chlorophenyl)ureido-1H-1,2,4-triazol-3-acetate 10 were synthesized. The obtained compounds were evaluated for their anti-inflammatory. Most of the tested compounds exhibited significant anti-inflammatory activities with compounds 9a-j were better than indomethacin. None of the tested compounds showed significant antitumor activity. Finally docking of selected compounds was performed to COX-2 and COX-1 enzymes in order to rationalize the obtained anti-inflammatory results and to predict the selectivity of the synthesized compounds.