(-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor
Published
Journal Article
Previous SAR studies of C-3 side chain modified analogs of (-)-SCH 48461, as well as information concerning the metabolic stability this series, enabled us to design a cholesterol absorption inhibitor (i.e., (-) 2a, SCH 57939) with tenfold higher potency and greatly enhanced metabolic stability. The synthesis and pharmacological profile, including the role of relative stereochemistry at both the C3 and 1' positions in determining the SAR of these compounds, will be discussed.
Full Text
Duke Authors
Cited Authors
- Kirkup, MP; Rizvi, R; Shankar, BB; Dugar, S; Clader, JW; McCombie, SW; Lin, SI; Yumibe, N; Huie, K; Van Heek, M; Compton, DS; Davis, HR; McPhail, AT
Published Date
- September 3, 1996
Published In
Volume / Issue
- 6 / 17
Start / End Page
- 2069 - 2072
International Standard Serial Number (ISSN)
- 0960-894X
Digital Object Identifier (DOI)
- 10.1016/0960-894X(96)00365-4
Citation Source
- Scopus