Anti-inflammatory, analgesic and antipyretic 4,6-disubstituted 3-cyanopyridine-2-ones and 3-cyano-2-aminopyridines
作者:F Manna、F Chimenti、A Bolasco、A Filippelli、A Palla、W Filippelli、E Lampa、R Mercantini
DOI:10.1016/0223-5234(92)90141-m
日期:1992.9
3-Cyano-4-(RR'-aryl)-6(2-hydroxyphenyl)-2-(1H)pyridones 2a-o and 3-cyano-4-(R-R'-aryl)-6-(2-hydroxyphenyl)-2-aminopyridines were synthesized which showed anti-inflammatory and analgesic activity. Electron withdrawing substituents in 2' or 4' position on 4-aryl group of compounds 2 increased the anti-inflammatory activity, while their displacement in the 3' position produced an increase of analgesic activity and the appearance of an edematous reaction. All compounds showed low antipyretic and antimicrobial activity. The compounds 2b, 2d, 2i, 2m and 2o did not show any interesting activity in the beta-adrenolytic, antihypertensive and heart frequency tests.