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.
Affiliations
- 1. BioCrea GmbH, Meissner Strasse 191, 01445 Radebeul, Germany. [email protected]
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.