Diarylpropane-1,3-dione Derivatives as TetR-Inducing Tetracycline Mimetics: Synthesis and Biological Investigations (pages 2924–2933)
Christian Kormann, Irina Pimenta, Stefan Löber, Cornelius Wimmer, Harald Lanig, Timothy Clark, Wolfgang Hillen and Peter Gmeiner
Version of Record online: 2 NOV 2009 | DOI: 10.1002/cbic.200900564
Cutting down on the essential: The β-diketone structure of tetracycline is known to chelate MgII to form a metal complex, which has been proven to be the TetR inducing agent. We designed novel, de novo TetR binders on 1,3-diaryl substituted β-diketones that retain this key structural motif. The introduction of additional tetracycline functional groups of gave insights into the structure–activity relationships of TetR induction and antibiotic potency.