Title of article
Novel 4-piperidinopyridine inhibitors of oxidosqualene cyclase-lanosterol synthase derived by consideration of inhibitor pKa
Author/Authors
George R. Brown، نويسنده , , Alan J. Foubister، نويسنده , , Michael C. Johnson، نويسنده , , Nicholas J. Newcombe، نويسنده , , David Waterson، نويسنده , , Stuart L. Wells، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
4
From page
2213
To page
2216
Abstract
Potent inhibition of rat microsomal oxidosqualene cyclase-lanosterol synthase (OSC) was maintained after structural modification of the 4-piperidinopyridine OSC inhibitor series. These novel analogues with a much lower pKa range (5.8–6.7) gave potent oral inhibition of rat cholesterol biosynthesis (8 ED80 0.7 mg/kg), and diminished effects on rat feeding after a 100 mg/kg oral dose.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791601
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