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Abstract

Spacer/linker based synthesis and biological evaluation of mutual prodrugs as antiinflammatory agents

Author(s): VS Velingkar, DR Jain, DC Ahire
Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, India

Correspondence Address:
V S Velingkar Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, India E-mail: [email protected]


Mutual prodrugs of some antiinflammatory agents were synthesized with the aim of improving the therapeutic index through prevention of gastrointestinal complications and to check the efficiency of release of the parent drug in presence of spacer. These mutual prodrugs were synthesized by direct condensation method using dicyclohexyl carbodiimide as a coupling agent and glycine as a spacer. The title compounds were characterized by spectral techniques and the release of the parent drug from mutual prodrug was studied in two different non-enzymatic buffer solutions at pH 1.2, pH 7.4 and in 80% human plasma. All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma. Biological activity of title compounds was studied by carrageenan-induced paw edema method. From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

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