Potential antiatherosclerotic agents. 6. Hypocholesterolemic trisubstituted urea analogues.
The discovery that a series of N,N-dialkyl-N'-arylureas were inhibitors of the ACAT enzyme has led to a structure-activity study involving the systematic modification of three sites of the urea backbone. This study culminated in the selection of N'-(2,4-dimethylphenyl)-N-benzyl-N-n-butylurea (115) for more extensive biological evaluation. ACAT inhibitors are seen as potentially beneficial agents against hypercholesterolemia and atherosclerosis.
DeVries
V G
VG
Medical Research Division, American Cyanamid Company, Lederle Laboratories, Pearl River, New York 10965.
Bloom
J D
JD
Dutia
M D
MD
Katocs
A S
AS
Largis
E E
EE
D000311:Adrenal Glands / Q000201:enzymology; D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis*; D001013:Aorta, Thoracic / Q000201:enzymology; D001161:Arteriosclerosis / Q000517:prevention & control*; D002478:Cells, Cultured; D002522:Chlorocebus aethiops; D004036:Diet, Atherogenic; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D008297:Male; D015394:Molecular Structure; D009131:Muscle, Smooth, Vascular / Q000201:enzymology; D011817:Rabbits; D051381:Rats; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*; D013261:Sterols / Q000378:metabolism; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use
D000924:Anticholesteremic Agents; D013261:Sterols; D014508:Urea; D002785:Sterol O-Acyltransferase