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

Abdel-Alim Abdel-Alim Mohamed (Department of Pharm. Organic Chemistry, Faculty of Pharmacy, University of Assiut)
EI-Shorbagi Abdel-Nasser Ahmed (Department of Pharm. Organic Chemistry, Faculty of Pharmacy, University of Assiut)
Abdel-Moty Samia Galal (Department of Pharm. Organic Chemistry, Faculty of Pharmacy, University of Assiut)
Abdel-Allah Hajjaj Hassan Mohamed (Department of Pharm. Organic Chemistry, Faculty of Pharmacy, University of Assiut)
Publication Information
Archives of Pharmacal Research / v.28, no.6, 2005 , pp. 637-647 More about this Journal
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
Prodrugs; 5-ASA; SASP; Nicotinamide; Analgesic; Anti-inflammatory; Ulcerative colitis;
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Times Cited By Web Of Science : 5  (Related Records In Web of Science)
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