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The Pharmaceutical Society of Korea (대한약학회)
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Synthesis and Anti-Inflammatory Testing of Some New Compounds Incorporating 5-Aminosalicylic Acid (5-ASA) as Potential Prodrugs

  • Published : 2005.06.01
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Abstract

This work includes the synthesis of 15 final compounds (6a-h and 7b-h) as prod rugs of 5-ASA in the form of the acid itself, esters and amides linked by an amide linkage through a spacer to the endocyclic ring N of nicotinamide. Also, 15 new intermediate compounds were prepared. The target compounds (6b, 6f, 7b, and 7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, $LD_{50}$, in vivo and in vitro metabolism of compound 7f were determined.

Keywords

References

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