Abstract
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.
MeSH terms
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Aminosalicylic Acids / chemical synthesis*
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Aminosalicylic Acids / therapeutic use*
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Animals
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Arthritis / chemically induced
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Arthritis / drug therapy
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Colitis / chemically induced
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Colitis / drug therapy
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Colon / drug effects
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Colon / pathology
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Female
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Inflammatory Bowel Diseases / chemically induced
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Inflammatory Bowel Diseases / drug therapy*
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Male
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Peroxidase / metabolism
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Prodrugs / chemical synthesis*
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Prodrugs / therapeutic use*
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Rats
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Rats, Wistar
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Ulcer / drug therapy
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Ulcer / pathology
Substances
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Aminosalicylic Acids
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Prodrugs
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Peroxidase