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Synthesis of trigonelline and nicotinamide linked prodrugs of 5 –aminosalicylic acid (5-ASA) with analgesic and anti-inflammatory effects

Research Authors
H. H. M. Abdu-Allah, A. M. Abdel-Alim, S. G. Abdel-Moty, A. A. El-Shorbagi
Research Date
Research Journal
Bulletin of Pharmaceutical Sciences Assiut University
Research Vol
28 (2)
Research Website
https://bpsa.journals.ekb.eg/article_65398.html
Research Year
2005
Research_Pages
237-253
Research Abstract

3-N-(4`-Hydroxy-3`-substituted phenyl)carbamoyl-1-methylpyridinium iodides (compds. 5b-j) and 3-carbamoyl-1-(N-(4`-hydroxy- 3`-substituted phenyl)carbamoyl) methyl pyridinium chlorides (compds. 7a-j) were synthesised and some of them were tested for their analgesic and antiinflammatory activities by hot plate test and carageenin-induced hind paw edema model, respectively. Compound 5b revealed the most potent analgesic and anti-inflammatory activities in comparison to sulfasalazine (SASP) and 5-ASA. In addition, ulcerogenicity, LD50, in-vivo and in vitro cleavage and pH stability of compound 5b were also determined.