Synthesis and anti-inflammatory testing of some new compounds incorporating 5 –aminosalicylic acid (5-ASA) as potential prodrugs

Faculty of Pharmacy

Assiut University

Synthesis and anti-inflammatory testing of some new compounds incorporating 5 –aminosalicylic acid (5-ASA) as potential prodrugs

Research Authors
Abdel-Alim, Abdel-Alim Mohamed; El-Shorbagi, Abdel-Nasser Ahmed; Abdel-Moty, Samia Galal; Abdel-Allah, Hajjaj Hassan Mohamed
Research Date
Research Department
Department of Pharmaceutical Organic Chemistry
Research Journal
Archives of Pharmacal Research
Research Publisher
Springer
Research Vol
28 (6)
Research Website
https://link.springer.com/article/10.1007%2FBF02969351
Research Year
2005
Research Member
Hajjaj Hassan Mohamed Abdu-Allah
Research_Pages
637-647
Research Abstract

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.