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Abdel-Alim Abdel-Alim Mohamed,EI-Shorbagi Abdel-Nasser Ahmed,Abdel-Moty Samia Galal,Abdel-Allah Hajjaj Hassan Mohamed The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.6
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.
Abdel-Alim Mohamed Abdel-Alim,Abdel-Nasser Ahmed El-Shorbagi,Samia Galal Abdel-Moty,Hajjaj Hassan Mohamed Abdel-Allah 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.6
This work includes the synthesis of 15 final compounds (6a-h and 7b-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, and 7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, LD50, in vivo and in vitro metabolism of compound 7f were determined.