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  • Title: Synthesis, biological and medicinal significance of S-glycosido-thieno[2,3-d]-pyrimidines as new anti-inflammatory and analgesic agents.
    Author: Hafez HN, El-Gazzar AR, Nawwar GA.
    Journal: Eur J Med Chem; 2010 Apr; 45(4):1485-93. PubMed ID: 20116903.
    Abstract:
    Several 2-thioglycosides were prepared. Glycosylation of 2-thioxo-thieno[2,3-d]-pyrimidines 5a,b with 1-bromo-2,3,5-tri-O-acetyl-alpha-d-arabinofuranosyle 7, 2,3,4,6-tetra-O-acetyl-alpha-d-glucopyranosyl and galacto-pyranosyl bromide 8a,b gave the protected beta-d-nuclosides 10a,b and 13a-d in high yields, which were transformed to deacetylated derivatives 14a,b and 15a-d. The structures of the compounds were elucidated by spectral and elemental analysis. Anti-inflammatory and Analgesic activities screening of the new compounds (at a dose of 100 mg/kg body weight) utilizing in vivo acute carrageenan-induced paw oedema standard method exhibited that the deacetylated derivatives 14a,b and 15a-d possess highly promising activities.
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