TETRAZOLE-SUBSTITUTED UREAS AS INHIBITORS OF ACYL-COA-CHOLESTEROL O-ACYLTRANSFERASE (ACAT) - A NOVEL PREPARATION OF UREAS FROM WEAKLY NUCLEOPHILIC AMINES

Authors
PURCHASE CF WHITE AD ANDERSON MK BOCAN TMA BOUSLEY RF HAMELEHLE KL HOMAN R KRAUSE BR LEE P MUELLER SB SPEYER C STANFIELD RL REINDEL JF
Citation
Cf. Purchase et al., TETRAZOLE-SUBSTITUTED UREAS AS INHIBITORS OF ACYL-COA-CHOLESTEROL O-ACYLTRANSFERASE (ACAT) - A NOVEL PREPARATION OF UREAS FROM WEAKLY NUCLEOPHILIC AMINES, Bioorganic & medicinal chemistry letters, 6(15), 1996, pp. 1753-1758
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
15
Year of publication
1996
Pages
1753 - 1758
Database
ISI
SICI code
0960-894X(1996)6:15<1753:TUAIOA>2.0.ZU;2-C
Abstract
A novel series of tetrazole-substituted ureas 2 were prepared from wea kly nucleophilic amines using a new coupling method. The ureas were fo und to potently inhibit liver ACAT in vitro and lower total serum chol esterol in vivo. A comparison of urea 2b and the anti-atherosclerotic CI-976 in a long-term model of atherosclerosis indicates the importanc e of inhibiting arterial ACAT for reducing lesion size. Copyright (C) 1996 Elsevier Science Ltd