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Bioorg Med Chem Lett. 2009 Jun 15;19(12):3174-6. doi: 10.1016/j.bmcl.2009.04.121. Epub 2009 May 3.

Discovery of selective PDE4B inhibitors.

Author information

1
Pharmaceuticals Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan.

Abstract

In this study the first PDE4B selective inhibitor is described. Optimization of lead 2-arylpyrimidine derivatives afforded a series of potent PDE4B inhibitors with >100-fold selectivity over the PDE4D isozyme. With a good pharmacokinetic profile, a selected compound exhibited potent anti-inflammatory effects in vivo and showed less emesis compared with Cilomilast.

PMID:
19447034
DOI:
10.1016/j.bmcl.2009.04.121
[Indexed for MEDLINE]

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