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Synthesis and Evaluation of Prodrug of 2-Acetoxybenzoic Acid with Amino-Acids
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2-Acetoxybenzoic acid suffers from the general side effects of NSAIDs, owing to presence of free carboxylic acid group. The study was aimed to retard the adverse effects of gastrointestinal origin. 4 prodrugs of 2-Acetoxybenzoic acid were synthesized by amidation with ethyl esters of amino acids, namely, glycine, L-phenylalanine, L-glutamic acid, L-aspartic acid. Purified synthesized prodrugs were characterized by m.p., TLC, solubility, elemental analyses, UV, FTIR, NMR. Synthesized prodrugs were subjected for Antypyretic, Analgesic, Anti-inflammatory activities and Ulcerogenic index. Marked reduction of ulcerogenic index and comparable Antypyretic, Analgesic, Anti-inflammatory activities were obtained in all cases as compared to 2-Acetoxybenzoic acid.
Keywords
Prodrugs, Bioavailability, Physical Characterization, Pharmacokinetics, Pharmacodyanamics.
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