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Amide conjugates of flurbiprofen with various amino acid methyl esters were synthesized by Schotten-Baumann technique using prodrug concept. Their physico-chemical characterization was carried out by analytical and spectral methods.They were subjected to in vitro hydrolysis in hydrochloric acid buffer (pH 1.2), phosphate buffer (pH 7.4) and 80% human plasma (pH 7.4).The amides were screened for analgesic, antiinflammatory and ulcerogenic activities. They showed comparable analgesic and antiinflammatory activities with appreciable decrease in the ulcer index. Amide conjugate of flurbiprofen with phenylalanine was found to be the most active, even more than the parent drug flurbiprofen.
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Author(s): Neha Gairola Deepika Nagpal Suneela S Dhaneshwar S R Dhaneshwar S C Chaturvedi