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

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Abstract
Benzoylacetonitrile and .beta.-aminocinnamonitrile possess potent antiinflammatory activity in the rat adjuvant arthritis model. In a series of phenyl-substituted analogs, 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.