(-)-SCH-57939 - SYNTHESIS AND PHARMACOLOGICAL PROPERTIES OF A POTENT,METABOLICALLY STABLE CHOLESTEROL ABSORPTION INHIBITOR

Authors
KIRKUP MP RIZVI R SHANKAR BB DUGAR S CLADER JW MCCOMBIE SW LIN SI YUMIBE N HUIE K VANHEEK M COMPTON DS DAVIS HR MCPHAIL AT
Citation
Mp. Kirkup et al., (-)-SCH-57939 - SYNTHESIS AND PHARMACOLOGICAL PROPERTIES OF A POTENT,METABOLICALLY STABLE CHOLESTEROL ABSORPTION INHIBITOR, Bioorganic & medicinal chemistry letters, 6(17), 1996, pp. 2069-2072
Citations number
9
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
17
Year of publication
1996
Pages
2069 - 2072
Database
ISI
SICI code
0960-894X(1996)6:17<2069:(-SAPP>2.0.ZU;2-A
Abstract
Previous SAR studies of C-3 side chain modified analogs of (-)-SCH 484 61,(1,3,4) as well as information concerning the metabolic stability t his series, enabled us to design a cholesterol absorption inhibitor (i .e., (-) 2a, SCH 57939) with tenfold higher potency and greatly enhanc ed metabolic stability. The synthesis and pharmacological profile, inc luding the role of relative stereochemistry at both the C3 and 1' posi tions in determining the SAR of these compounds, will be discussed. Co pyright (C) 1996 Elsevier Science Ltd