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G. Y. Paris, D. L. Garmaise, D. G. Cimon, L. Swett, G. W. Carter and P. Young, “Glycerides as Prodrugs: Synthesis and Antiinflammatory Activity of 1,3-Bis(alkanoyl)-2-(O-acetylsalicyloy) Glycerides (Aspirin Triglycerides),” Journal of Medicinal Chemistry Vol. 22, No. 6, 1979, pp. 683-687. doi:10.1021/jm00192a014

has been cited by the following article:

• TITLE: Synthesis and Evaluation of Glyceride Prodrugs of Naproxen

  AUTHORS: Vivekkumar K. Redasani, Sanjay B. Bari

  KEYWORDS: Naproxen; Glyceride Prodrugs; Anti-Inflammatory; Analgesic; Gastroprotective; Hydrolysis Kinetics

  JOURNAL NAME: Open Journal of Medicinal Chemistry, Vol.3 No.3, September 20, 2013

  ABSTRACT: The glyceride ester derivatives 6a and 6b were prepared by reacting 1,2,3-trihydroxy propane 1,3-dipalmitate/stearate with (S)-naproxen as potential prodrugs. The synthesis was achieved successfully with the aid of N,N’-dicyclohexyl- carbodiimide. These prodrugs were evaluated for anti inflammatory, analgesic and gastroprotective activity. It was found that prodrugs 6a and 6b showed less irritation to gastric mucosa as indicated by ulcer index. The synthesized glyceride esters were found to possess good pharmacological profile as shown by results of anti inflammatory and analgesic activity. The aqueous studies were performed in order to ensure the release of prodrugs. Both prodrugs were found to stable at acidic pH while undergoes hydrolysis at pH 7.4. These findings suggest that the glyceride prodrugs 6a and 6b might be used as potential biolabile derivatives.