CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF PYRIPYROPENES .2. 1,11-CYCLIC ANALOGS

Authors
OBATA R SUNAZUKA T KATO Y TOMODA H HARIGAYA Y OMURA S
Citation
R. Obata et al., CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF PYRIPYROPENES .2. 1,11-CYCLIC ANALOGS, Journal of antibiotics, 49(11), 1996, pp. 1149-1156
Citations number
6
Categorie Soggetti
Pharmacology & Pharmacy",Immunology,"Biothechnology & Applied Migrobiology
Journal title
Journal of antibiotics → ACNP
ISSN journal
00218820
Volume
49
Issue
11
Year of publication
1996
Pages
1149 - 1156
Database
ISI
SICI code
0021-8820(1996)49:11<1149:CMASOP>2.0.ZU;2-E
Abstract
A series of 1,11-cyclic analogs of pyripyropene A were prepared. Repla cement of the 1,11-acyl groups of pyripyropenes with 1,11-cyclic aceta ls effectively improved in vitro acyl CoA:cholesterol acyltransferase (ACAT) inhibitory activity. Especially noteworthy is benzylidene aceta l analog 35, the most potent inhibitor (IC50 = 5.6 nM) among the deriv atives prepared so far, which showed 16 times more potent inhibitory a ctivity than pyripyropene A.