Synthesis of 3-Ureido Derivatives of Coumarin and 2-Quinolone as Potent Acyl-CoA : Cholesterol Acyltransferase Inhibitors

Novel 3-ureido derivatives of 4-phenylcoumarin and 4-phenyl-2-quinolone were synthesized and evaluated for acyl-CoA : cholesterol acyltransferase (ACAT)-inhibitory activity. These derivatives inhibited rat intestinal ACAT with IC50 values at the 10-8 to 10-9 M level and were found to normalize plasm...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1995/04/15, Vol.43(4), pp.616-625
Hauptverfasser:	TAWADA, Hiroyuki, NATSUGARI, Hideaki, ISHIKAWA, Eiichiro, SUGIYAMA, Yasuo, IKEDA, Hitoshi, MEGURO, Kanji
Format:	Artikel
Sprache:	eng
Schlagworte:	ACAT inhibitor Animals antiatherosclerotic agent Biological and medical sciences cholesterol esterification Coumarins - chemical synthesis Coumarins - chemistry Coumarins - pharmacology General and cellular metabolism. Vitamins hypocholesterolemic effect Hypolipidemic Agents - pharmacology In Vitro Techniques Magnetic Resonance Spectroscopy Male Medical sciences Pharmacology. Drug treatments Quinolones - chemical synthesis Quinolones - chemistry Quinolones - pharmacology Rats Rats, Sprague-Dawley Sterol O-Acyltransferase - antagonists & inhibitors ureidocoumarin ureidoquinolone
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Zusammenfassung:	Novel 3-ureido derivatives of 4-phenylcoumarin and 4-phenyl-2-quinolone were synthesized and evaluated for acyl-CoA : cholesterol acyltransferase (ACAT)-inhibitory activity. These derivatives inhibited rat intestinal ACAT with IC50 values at the 10-8 to 10-9 M level and were found to normalize plasma cholesterol levels in cholesterol-fed rats when administered as dietary admixtures.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.43.616