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

R Gewald, C Grunwald, U Egerland

Index: Gewald, Rainer; Grunwald, Christian; Egerland, Ute Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 15 p. 4308 - 4314

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Citation Number: 14

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.