Bioorganic and Medicinal Chemistry Letters p. 2069 - 2072 (1996)
Update date:2022-08-05
Topics:
Kirkup, Michael P.
Rizvi, Razia
Shankar, Bandarpalle B.
Dugar, Sundeep
Clader, John W.
McCombie, Stuart W.
Lin, Sue-Ing
Yumibe, Nathan
Huie, Keith
Van Heek, Margaret
Compton, Douglas S.
Davis Jr., Harry R.
McPhail, Andrew T.
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.
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