2. Academic Validation
  3. Discovery of triazines as potent, selective and orally active PDE4 inhibitors

Discovery of triazines as potent, selective and orally active PDE4 inhibitors

  • Bioorg Med Chem Lett. 2013 Aug 1;23(15):4308-14. doi: 10.1016/j.bmcl.2013.05.099.
Rainer Gewald 1,  Christian Grunwald,  Ute Egerland
Affiliations

Affiliation

  • 1 BioCrea GmbH, Meissner Strasse 191, 01445 Radebeul, Germany. rainer.gewald@telecolumbus.net
PMID: 23806553 DOI: 10.1016/j.bmcl.2013.05.099
Abstract

Expanding on HTS hit 4 afforded a series of [1,3,5]triazine derivatives as novel PDE4 inhibitors. The SAR development and optimization process with the emphasis on ligand efficiency and physicochemical properties led to the discovery of compound 44 as a potent, selective and orally active PDE4 Inhibitor.

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