European Journal of Medicinal Chemistry 2009-10-01

Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.

Suneela S Dhaneshwar, Neha Gairola, Mini Kandpal, Gaurav Vadnerkar, Lokesh Bhatt, Badal Rathi, S S Kadam

文献索引：Eur. J. Med. Chem. 44 , 3922-9, (2009)

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摘要

Colon-specific mutual azo prodrugs of 5-aminosalicylic acid with essential amino acids were synthesized for the management of inflammatory bowel disease. The structures were confirmed by elemental and spectral analyses. 85-88% release of 5-aminosalicylic acid was achieved in rat fecal matter with half-lives ranging from 140 to 160 min, following first order kinetics. The prodrugs exhibited comparable ameliorating effect as that of sulfasalazine on trinitrobenzenesulfonic acid-induced experimental colitis in rats with a better safety profile.