Discovery of oral and inhaled PDE4 inhibitors.

Bioorg Med Chem Lett

Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA. Electronic address:

Published: October 2013

The optimization of oxazole-based PDE4 inhibitor 1 has led to the identification of both oral (compound 16) and inhaled (compound 34) PDE4 inhibitors. Selectivity against PDE10/PDE11, off target screening, and in vivo activity in the rat are discussed.

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http://dx.doi.org/10.1016/j.bmcl.2013.08.056DOI Listing

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