Citation
W. Vaccaro et al., INHIBITORS OF ACYL COA-CHOLESTEROL ACYLTRANSFERASE, Journal of medicinal chemistry, 39(8), 1996, pp. 1704-1719
Citations number
19
Categorie Soggetti
Chemistry Medicinal
Journal title
ISSN journal
00222623
Volume
39
Issue
8
Year of publication
1996
Pages
1704 - 1719
Database
ISI
SICI code
0022-2623(1996)39:8<1704:IOACA>2.0.ZU;2-S
Abstract
Conformational restriction of previously disclosed acyclic diphenyleth
yl)diphenylacetamides led to the discovery of several potent inhibitor
s of acyl CoA:cholesterol acyltransferase (ACAT). s-[2-(4-Hydroxypheny
l)-1-indanyl]diphenylacetamide (4a) was the mo st potent ACAT inhibito
r identified (IC50 = 0.04 mu M in an in vitro rat hepatic microsomal A
CAT assay, ED(50) = 0.72 mg/kg/day in cholesterol-fed hamsters).