Antiinflammatory agents. 4. Syntheses and biological evaluation of potential pro-drugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl) …
…, DA Shamblee, WJ Welstead Jr, JC Nolan…
文献索引：Walsh, David A.; Moran, H. Wayne; Shamblee, Dwight A.; Welstead, William J.; Nolan, Joseph C.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 8 p. 2296 - 2304
A series of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid (amfenac) and 2- amino-3-(4-chlorobenzoy1) benzeneacetic acid were synthesized and evaluated for their cyclooxygenase inhibiting properties, antiinflammatory potency, and gastrointestinal irritation liability. One compound, 2-amino-3-(4-chlorobenzoyl)-benzeneacetamide. possessed a therapeutic index 1 order of magnitude greater than that of indomethacin.
