title: Xanthone analogues of clofibrate / Synthesis and biological evaluation as antagonists of lipolysis in vitro.
abstract: By appropriate superimposing of fenofibrate and fenofibric acid molecules, two xanthone derivatives (closed models) may be obtained. These compounds as well as their four chlorine-free isomers were prepared and tested on adrenaline- and theophylline-induced lipolysis in rat fat cells in comparison with ethyl 2-(4-chlorophenoxy)-2-methylpropionate (clofibrate). Some of these new derivatives besides being good inhibitors of adrenaline effect, as clofibrate is, were also very active in reducing theophylline-induced lipolysis. Very promising for further studies is the chlorine-free 3-isomer (3e). The possible difference in the action mechanism of these compounds as compared with clofibrate and the structure-activity relationships are briefly discussed.
mesh_terms: D000273:Adipose Tissue / Q000378:metabolism; D000818:Animals; D002478:Cells, Cultured; D002994:Clofibrate / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004837:Epinephrine / Q000494:pharmacology; D008066:Lipolysis / Q000187:drug effects*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013806:Theophylline / Q000494:pharmacology
chemical_list: D013806:Theophylline; D002994:Clofibrate; D004837:Epinephrine