Synthesis and hypolipidemic activity of diesters of arylnaphthalene lignan and their heteroaromatic analogs.
A series of diesters of arylnaphthalene lignan and their heteroaromatic analogs were synthesized and evaluated for hypolipidemic activity. The disasters with modifications at C-3 showed excellent hypocholesterolemic and high-density lipoprotein (HDL) cholesterol-elevating activities. Structure-activity analysis indicated that the 2-pyridylmethyl ester 5l has the optimum activity.
Kuroda
T
T
Research Laboratories of Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Kondo
K
K
Iwasaki
T
T
Ohtani
A
A
Takashima
K
K
D000818:Animals; D002784:Cholesterol / Q000097:blood; D008076:Cholesterol, HDL / Q000097:blood; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017705:Lignans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008055:Lipids / Q000097:blood*; D008297:Male; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D008076:Cholesterol, HDL; D000960:Hypolipidemic Agents; D017705:Lignans; D008055:Lipids; D009281:Naphthalenes; D002784:Cholesterol