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KMID : 0043320050280060637
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Archives of Pharmacal Research
2005 Volume.28 No. 6 p.637 ~ p.647
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Synthesis and Anti-Inflammatory Testing of Some New Compounds Incorporating 5-Aminosalicylic Acid (5-ASA) as Potential Prodrugs*
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Abdel-Alim Mohamed Abdel-Alim
Abdel-Nasser Ahmed El-Shorbagi
Samia Galal Abdel-Moty
Hajjaj Hassan Mohamed Abdel-Allah
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Abstract
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This work includes the synthesis of 15 final compounds (6a-h and7b-h) as prodrugs 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, and7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, LD50,in vivo andin vitro metabolism of compound7f were determined.
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KEYWORD
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Prodrugs, 5-ASA, SASP, Nicotinamide, Analgesic, Anti-inflammatory, Ulcerative colitis
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