N-HYDROXYGLYCINE DERIVATIVES AS NOVEL INHIBITORS OF SQUALENE SYNTHASE

Authors
WATTANASIN S BOETTCHER BR SCALLEN T
Citation
S. Wattanasin et al., N-HYDROXYGLYCINE DERIVATIVES AS NOVEL INHIBITORS OF SQUALENE SYNTHASE, Bioorganic & medicinal chemistry letters, 7(23), 1997, pp. 3039-3044
Citations number
20
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
23
Year of publication
1997
Pages
3039 - 3044
Database
ISI
SICI code
0960-894X(1997)7:23<3039:NDANIO>2.0.ZU;2-M
Abstract
The squalene synthase inhibiting properties of farnesyl diphosphate (F PP) mimics, 3 and related analogues, are described. The results indica te that the nonphosphorus-containing N-hydroxyglycine is a novel repla cement for the diphosphate group. Further optimization of 3 has led to 12, a new and potent squalene synthase inhibitor. (C) 1997 Elsevier S cience Ltd.