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Published on: January 7, 2019
Dibenzodioxocinones--a new class of CETP inhibitors
David Brückner1, Frank-Thorsten Hafner, Volkhart Li
1Bayer Healthcare Pharma Research, Aprather Weg, 42096 Wuppertal, Germany.
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.
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