INHIBITION OF OXIDOSQUALENE CYCLASE BY SUBSTITUTED QUINOLIZIDINES

Authors
MARQUART AL SCHATZMAN GL PEET NP MOORE WR HUBER EW GALLION SL ANGELASTRO MR
Citation
Al. Marquart et al., INHIBITION OF OXIDOSQUALENE CYCLASE BY SUBSTITUTED QUINOLIZIDINES, Bioorganic & medicinal chemistry letters, 4(11), 1994, pp. 1317-1318
Citations number
9
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
11
Year of publication
1994
Pages
1317 - 1318
Database
ISI
SICI code
0960-894X(1994)4:11<1317:IOOCBS>2.0.ZU;2-W
Abstract
Substituted hydroxyquinolizidines have been synthesized as conformatio nally restricted analogs of the type II high-energy intermediate forme d during the cyclization of 2,3-oxidosqualene to lanosterol. Compounds 4a and 4b were found to be potent inhibitors of rat liver oxidosquale ne cyclase (OSC) with K(i) values of 0.51 muM and 0.11 muM, respective ly.