• Picomolar FKBP inhibitors enabled by a single water-displacing methyl group in bicyclic [4.3.1] aza-amides 

      Kolos, Jürgen M; Pomplun, Sebastian; Jung, Sascha; Rieß, Benedikt; Purder, Patrick L; Voll, Andreas M; Merz, Stephanie; Gnatzy, Monika; Geiger, Thomas M; Quist-Løkken, Ingrid; Jatzlau, Jerome; Knaus, Petra; Holien, Toril; Bracher, Andreas; Meyners, Christian; Czodrowski, Paul; Krewald, Vera; Hausch, Felix (Journal article; Peer reviewed, 2021)
      Methyl groups can have profound effects in drug discovery but the underlying mechanisms are diverse and incompletely understood. Here we report the stereospecific effect of a single, solvent-exposed methyl group in bicyclic ...