Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
IMIDAZOLYLBENZOPYRANE DERIVATIVES - A NEW CLASS OF ACYL-COA - CHOLESTEROL ACYLTRANFERASE (ACAT) INHIBITORS
Autore:
FANCELLI D; CHIARI A; COZZI P; LOVISOLO P; SEVERINO D; GHISELLI G;
Indirizzi:
PHARM FARMITALIA CARLO ERBA RES INST,VIA PAPA GIOVANNI XXIII 23 I-20014 MILAN ITALY
Titolo Testata:
Journal of enzyme inhibition
fascicolo: 3, volume: 8, anno: 1994,
pagine: 159 - 172
SICI:
8755-5093(1994)8:3<159:ID-ANC>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
APO-B SECRETION; O-ACYLTRANSFERASE; ANTIATHEROSCLEROTIC ACTIVITY; HYPOCHOLESTEROLEMIC AGENTS; POTENT INHIBITORS; ABSORPTION; IDENTIFICATION; SERIES; CI-976; LIVER;
Keywords:
ACYL-COA- CHOLESTEROL ACYLTRANSFERASE; ACAT; INHIBITION; 2, 6-DISUBSTITUTED-3-IMIDAZOLYLBENZOPYRANES; ATHEROSCLEROSIS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
D. Fancelli et al., "IMIDAZOLYLBENZOPYRANE DERIVATIVES - A NEW CLASS OF ACYL-COA - CHOLESTEROL ACYLTRANFERASE (ACAT) INHIBITORS", Journal of enzyme inhibition, 8(3), 1994, pp. 159-172

Abstract

Inhibitors of the enzyme Acyl-CoA: Cholesterol Acyltransferase are regarded as potentially useful agents in the treatment of hypercholesterolemia and atherosclerosis. We report here a novel series of 2, 6-disubstituted-3-imidazolylbenzopyrane derivatives with significant in vitro ACAT inhibitory activity (IC50 range 0.05-0.5 mu M) Compounds of this series such as 26 are examples of a new, structurally distinct classof potent ACAT inhibitors with high specificity for the aortic subtype of the enzyme. The structure-activity relationships of the 3-imidazolylbenzopyrane ACAT inhibitors were investigated by systematic manipulation of two regions of the parent compound 1 and the inhibitory activity resulted linked to the substituent in position 6 of the benzopyrane ring and modulated by the size of lipophilic substituents in position 2. Investigation of the mechanism of the inhibitory effect leads to the conclusion that these compounds act in a non-competitive fashion.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 09:08:56