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Synthesis, Anti-inflammatory, Analgesic, and Antibacterial Activities of Some Triazole, Triazolothiadiazole, and Triazolothiadiazine Derivatives

مؤلف البحث
Mostafa A. Hussein, Refaat M. Shaker, Mohammed A. Ameen, Mohammed F. Mohammed
مجلة البحث
Arch. Pharm. Res, DOI 10.1007/s12272-011-0802-z.
تصنيف البحث
1
عدد البحث
Vol.34,No.8
سنة البحث
2011
المشارك في البحث
ملخص البحث

The current work is concerned with synthesis of new 1,2,4-traizoles, 1,3,4-thiadiazoles, and 1,3,4-thiadiazines derivatives. Derivatives 3a-i were obtained by condensation of 4-amino-3-(4-pyridine)-5-mercapto-1,2,4-triazole 1 with the appropriate aldehyde. Compounds 4a-i were synthesized in a one pot reaction involving compounds 3a-i, formaldehyde and morpholine. Condensation of compound 1 with the appropriate acids 4-substituted phenacyl bromide gave compounds 6a-d and 8a-f respectively. The chemical structures of the newly synthsized derivatives were elucidated using different spectral and elemental methods of analyses. All compounds were evaluated for their anti-inflammatory activity and the most potent derivatives were tested for their analgesic activity using indomethacin as a reference drug. In addition, ulcerogenicity and LD50 for the most active compounds were evaluated. Moreover, The antibacterial activities of the newly synthesized derivatives were investigated.