- Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues
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A series of substituted derivatives of 2-amino-3-benzoylphenylacetic acid (amfenac) has been synthesized and evaluated for antiinflammatory, analgesic, and cyclooxygenase inhibiting activity. Several derivatives including 4'-chloro, 4'-bromo and 5-chloro, 4'-bromo were more potent than indomethacin in these assays.
- Walsh,Moran,Shamblee,Uwaydah,Welstead Jr.,Sancilio,Dannenburg
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p. 1379 - 1388
(2007/10/02)
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- 4-(5- And 7-)benzoylindolin-2-ones and pharmaceutical uses thereof
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Novel 4-(5- and 7-)benzoylindolin-2-ones of the formula: SPC1 Wherein R is hydrogen, lower-alkyl, or methylthio, R1 is hydrogen or lower-alkyl, R2 is lower-alkyl, lower-alkoxy, halogen, nitro or trifluoromethyl, R3 is hydrogen, halogen or lower-alkoxy, and n is 0, 1 or 2, are prepared by (a) acylation of indolin-2-one to give 5-benzoylindoline-2-one, (b) cyclization of 2-acetamido-3-benzoylphenylacetic acid or ethyl 2-acetamido-3-benzoylphenylacetate to give 7-benzoyindoline-2-one, or (c) by reacting aminobenzophenones with alkyl α(methylthio)acetates to give alkyl 2-amino-3-(5- or 6-)benzoyl-α-(methylthio)phenylacetates which are cyclized and demethylthiolated to 4-(5- and 7-)benzoylindolin-2-ones. The novel compounds possess anti-inflammatory activity and are intermediates for the preparation of 2-amino-3-(5- or 6-) benzoylphenylacetic acids which posess anti-inflammatory properties.
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