Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid
| Autor: | Joseph C. Nolan, Dwight A. Shamblee, Gustav Graff, Moran Hw, L. F. Sancilio, David A. Walsh, William J. Welstead |
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| Rok vydání: | 1990 |
| Předmět: |
Male
Chemical Phenomena medicine.drug_class Gastrointestinal Diseases Indomethacin Benzeneacetamides Pharmacology Carrageenan Aminoketone chemistry.chemical_compound Therapeutic index Drug Discovery Acetamides medicine Potency Animals Cyclooxygenase Inhibitors Prodrugs Biological evaluation Phenylacetates Inflammation biology Molecular Structure Anti-Inflammatory Agents Non-Steroidal Prodrug Arthritis Experimental Rats Chemistry chemistry Enzyme inhibitor biology.protein Molecular Medicine Female Cyclooxygenase Amfenac |
| Zdroj: | Journal of medicinal chemistry. 33(8) |
| ISSN: | 0022-2623 |
| Popis: | A series of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid (amfenac) and 2-amino-3-(4-chlorobenzoyl) 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 |
| Databáze: | OpenAIRE |
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