(-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor

Journal Article (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