Polyunsaturated fatty acid anilides as inhibitors of acyl-CoA : cholesterol acyltransferase (ACAT)

Authors
Matsuyama, N Kosaka, T Fukuhara, M Soda, Y Mizuno, K
Citation
N. Matsuyama et al., Polyunsaturated fatty acid anilides as inhibitors of acyl-CoA : cholesterol acyltransferase (ACAT), BIOORG MED, 9(14), 1999, pp. 2039-2042
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
14
Year of publication
1999
Pages
2039 - 2042
Database
ISI
SICI code
0960-894X(19990719)9:14<2039:PFAAAI>2.0.ZU;2-K
Abstract
A series of polyunsaturated fatty acid anilides were synthesized and evalua ted as ACAT inhibitors. Compound 24 had potent inhibitory activity against microsomal ACAT derived from U937, HepG2 and Caco-2 cell lines. Therefore, it might be expected to act as an antiarteriosclerotic and hypocholesterole mic agent. Interestingly, the ACAT inhibitory potency of 24 varied signific antly depending on the source of the enzyme. (C) 1999 Elsevier Science Ltd. All rights reserved.