Title of article
Dibenzodioxocinones—A new class of CETP inhibitors
Author/Authors
David Brückner، نويسنده , , Frank-Thorsten Hafner، نويسنده , , Volkhart Li، نويسنده , , Carsten Schmeck، نويسنده , , Joachim Telser، نويسنده , , Alexandros Vakalopoulos، نويسنده , , Gabriele Wirtz، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
3611
To page
3614
Abstract
Derivatives of the natural product 11-hydroxy-3-[(S)-1-hydroxy-3-methylbutyl]-4-methoxy-9-methyl-5H,7H-dibenzo[b,g][1,5]dioxocin-5-one 1 were studied as novel CETP inhibitors. Compound 2 was identified from HTS as a micromolar inhibitor. The compound suffered from very low stability in plasma. Optimisation by partial synthesis started from 1 and led to low-nanomolar inhibitors with good stability in rat plasma.
Keywords
Dibenzodioxocinones , CETP
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795845
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