Arylnaphthalene lignans as novel series of hypolipidemic agents raising high-density lipoprotein level.
A series of arylnaphthalene lignans were synthesized and tested for hypolipidemic activity. The most potent compound (4b) (TA-7552) not only reduced serum cholesterol, but also increased high-density lipoproteins cholesterol in rats. The effective dose of 4b is 100 times less than that of cholestyramine. Structure-activity relationships are discussed.
Iwasaki
T
T
Research Laboratories of Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Kondo
K
K
Nishitani
T
T
Kuroda
T
T
Hirakoso
K
K
Ohtani
A
A
Takashima
K
K
D000818:Animals; D000924:Anticholesteremic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D008076:Cholesterol, HDL / Q000097:blood*; D006937:Hypercholesterolemia / Q000188:drug therapy; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D009284:Naphthols / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D000924:Anticholesteremic Agents; D008076:Cholesterol, HDL; D009284:Naphthols; C090176:TA 7552