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

IE Bylov; MV Vasylyev; YV Bilokin

doi:10.1016/s0223-5234(99)00119-1

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

Eur J Med Chem. 1999 Nov 1;34(11):997-1001. doi: 10.1016/s0223-5234(99)00119-1.

Authors

IE Bylov¹, MV Vasylyev, YV Bilokin

Affiliation

¹ Department of Organic Chemistry, Ukrainian Academy of Pharmacy, 310002, Kharkov, Ukraine

PMID: 10889323
DOI: 10.1016/s0223-5234(99)00119-1

Abstract

Aseries 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 evaluated for their anti-inflammatory activity in carrageenan-induced rat paw oedema assays and in acetic acid-induced peritonitis tests in albino rats. The resulting products were found to be active anti-inflammatory agents and their 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 studied at graded doses for their acute toxicity (ALD(50)) in albino mice and were essentially non-toxic at the highest dose tested.