CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF PYRIPYROPENES - POTENT, BIOAVAILABLE INHIBITOR OF ACYL-COA-CHOLESTEROL O-ACYLTRANSFERASE (ACAT)

Authors
OBATA R SUNAZUKA T TOMODA H HARIGAYA Y OMURA S
Citation
R. Obata et al., CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF PYRIPYROPENES - POTENT, BIOAVAILABLE INHIBITOR OF ACYL-COA-CHOLESTEROL O-ACYLTRANSFERASE (ACAT), Bioorganic & medicinal chemistry letters, 5(22), 1995, pp. 2683-2688
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
22
Year of publication
1995
Pages
2683 - 2688
Database
ISI
SICI code
0960-894X(1995)5:22<2683:CMASOP>2.0.ZU;2-E
Abstract
Modification and structure-activity relationships of ACAT inhibitor py ripyropene were examined. PR-109 (7g) showed the most potent (IC50 = 6 nM) inhibitory activity. PR-86 (2e) also had strong inhibitory activi ty (IC50 = 19 nM) and its in vivo activity improved 10 times better (E D(50) = 10 mg/kg) than that of pyripyropene A.