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Bioorg Med Chem Lett. 2013 Oct 15;23(20):5528-32. doi: 10.1016/j.bmcl.2013.08.056. Epub 2013 Aug 21.

Discovery of oral and inhaled PDE4 inhibitors.

Author information

  • 1Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA. Electronic address: pauline.ting@merck.com.

Abstract

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.

Copyright © 2013 Elsevier Ltd. All rights reserved.

KEYWORDS:

Asthma; COPD; PDE4 inhibitor

PMID:
24018187
[PubMed - indexed for MEDLINE]
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