Journal of Medicinal Chemistry p. 1385 - 1389 (1979)
Update date:2022-09-26
Topics:
Ridge
Hanifin
Harten
Johnson
Menschik
Nicolau
Sloboda
Watts
Benzoylacetonitrile and β-aminocinnamonitrile are shown to possess potent intiinflammatory 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-β-aminocinnamonitrile retained activity. Additionally, β-amino-2- and β-amino-3-thiopheneacrylonitrile and β-oxo-2- and β-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.
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Doi:10.1039/c0cc03367g
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