Synthesis and stability of two indomethacin prodrugs
Autor: | Robert Mack Riggs, Abeer M. Al-Ghananeem, Peter A. Crooks, Shyamala Chandrasekaran |
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Rok vydání: | 2005 |
Předmět: |
Magnetic Resonance Spectroscopy
Stereochemistry Clinical Biochemistry Indomethacin Pharmaceutical Science Cleavage (embryo) Biochemistry Chemical synthesis Medicinal chemistry chemistry.chemical_compound Hydrolysis Amide Enzymatic hydrolysis Drug Discovery Moiety Prodrugs Molecular Biology Chromatography High Pressure Liquid Organic Chemistry Anti-Inflammatory Agents Non-Steroidal Prodrug Hydrogen-Ion Concentration chemistry Molecular Medicine Spectrophotometry Ultraviolet Conjugate |
Zdroj: | Bioorganicmedicinal chemistry letters. 16(7) |
ISSN: | 0960-894X |
Popis: | The purpose of this study was to synthesize and study the in vitro enzymatic and non-enzymatic hydrolysis of indomethacin–TEG ester and amide prodrugs. It was found that the ester conjugate 10 was comparatively stable between pH 3 and 6 (half-life >90 h), with a half-life equal to 5.2 h in 80% buffered plasma. In contrast, the amide conjugate 12 appeared to be stable over the entire pH range studied with the only observed degradation being cleavage of the indolic N -4-chlorobenzoyl moiety. |
Databáze: | OpenAIRE |
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