Author/Authors :
Michael P. Kirkup، نويسنده , , Razia Rizvi، نويسنده , , Bandarpalle B. Shankar، نويسنده , , Sundeep Dugar، نويسنده , , John W. Clader، نويسنده , , Stuart W. McCombie، نويسنده , , Sue-Ing Lin، نويسنده , , Nathan Yumibe، نويسنده , , Keith Huie، نويسنده , , Margaret Van Heek، نويسنده , , Douglas S. Compton، نويسنده , , Harry R. Davis Jr.، نويسنده , , Andrew T. McPhail، نويسنده ,
Abstract :
Previous SAR studies of C-3 side chain modified analogs of (−)-SCH 48461, 1,3,4as 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.
