| Literature DB >> 15975789 |
David Brückner1, Frank-Thorsten Hafner, Volkhart Li, Carsten Schmeck, Joachim Telser, Alexandros Vakalopoulos, Gabriele Wirtz.
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.Entities:
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Year: 2005 PMID： 15975789 DOI： 10.1016/j.bmcl.2005.05.073
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823