Synthesis and anti-inflammatory activity of N-substituted 2-oxo-2H-1-benzopyran-3-carboxamides and their 2-iminoanalogues

A series of N-arylsubstituted 2-imino-2H-1-benzopyran-3-carboxamides 3a and b and 2-oxo-2H-1-benzopyran-3-carboxamides 4a-h were synthesized and evalu ated for their anti-inflammatory activity in carrageenan-induced rat paw oe dema assays and in acetic acid-induced peritonitis tests in albino rats. Th e resulting products were found to be active anti-inflammatory agents and t heir effects were comparable to that of piroxicam as the reference compound . In the consideration of the efficacy of the compounds in these assays, 2- imino/oxo-2H-1-benzopyran-3-carboxamides 3a and b and 4a-h were further stu died at graded doses for their acute toxicity (ALD(50)) in albino mice and were essentially non-toxic at the highest dose tested. (C) 1999 Editions sc ientifiques et medicales Elsevier SAS.