2(5H)-FURANONES SUBSTITUTED IN THE 3 POSITION, AS Ca2+ CHANNEL ANTAGONISTS AND ANTI-INFLAMMATORY AGENTS

摘要

Compounds of formula (1), in which R is alkyl, arylalkyl or substituted arylalkyl, or alkenyl containing one or more olephinic bond; X is O, NH or NR1, where R1 is alkyl of 1 to 20 carbons or arylalkyl; and Y is H, alkyl of 1 to 20 carbons, arylalkyl, aryl, substituted aryl, substituted arylalkyl, alkenyl containing one or more olephinic bonds, PO(OH)2, PO(OH)OR2, PO(OH)R2, PO(OR2)2, where R2 is independently alkyl of 1 to 20 carbons, phenyl, or substituted phenyl, further Y is CO-R3, CO-OR3, CONHR3, SO2R3, SO2NHR3, (CH2)n-O-R3, or (CH2)n-O-(CH2)m-O-R3, where n, and m, are integers and are independently 1 to 20 and R3 is H, alkyl, alkenyl containing one or more olephinic bonds, aryl, substituted aryl, arylalkyl or substituted arylalkyl, with the proviso that when Y is CO-R3, CO-OR3, and CONHR3 then R3 is not hydrogen, are disclosed. The compounds are Ca2+ channel antagonist, have weak or no activity as inhibitors of phospholipase A¿2?, and are anti-inflammatory agents.