Potential antiarthritic agents. 2. Benzoylacetonitriles and .beta.-aminocinnamonitriles

Benzoylacetonitrile and beta-aminocinnamonitrile are shown to possess potent antiinflammatory activity in the rat adjuvant arthritis model. In a series of phenyl-substituted analogues, only o-, m-, and p-fluorobenzoylacetonitrile and m- and p-fluoro-beta-aminocinnamonitrile retained activity. Additi...

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Veröffentlicht in:	Journal of medicinal chemistry 1979-11, Vol.22 (11), p.1385-1389
Hauptverfasser:	Ridge, David N, Hanifin, J. William, Harten, Linda A, Johnson, Bernard D, Menschik, Judith, Nicolau, Gabriela, Sloboda, Adolph E, Watts, Doris E
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetonitriles - chemical synthesis Acetonitriles - metabolism Acetonitriles - pharmacology Acetonitriles - therapeutic use Animals Anti-Inflammatory Agents - chemical synthesis Arthritis, Experimental - drug therapy Edema - drug therapy Erythema - drug therapy Guinea Pigs Nitriles - chemical synthesis Nitriles - pharmacology Nitriles - therapeutic use Rats Structure-Activity Relationship
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Zusammenfassung:	Benzoylacetonitrile and beta-aminocinnamonitrile are shown to possess potent antiinflammatory activity in the rat adjuvant arthritis model. In a series of phenyl-substituted analogues, only o-, m-, and p-fluorobenzoylacetonitrile and m- and p-fluoro-beta-aminocinnamonitrile retained activity. Additionally, beta-amino-2- and beta-amino-3-thiopheneacrylonitrile and beta-oxo-2- and beta-oxo-3-thiophenepropionitrile exhibited similar activity. These agents are not believed to be acting via prostaglandin synthetase inhibition. The metabolic profile of benzoylacetonitrile is also described.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00197a020