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Bioorg Med Chem Lett. 2015 Feb 1;25(3):649-53. doi: 10.1016/j.bmcl.2014.11.090. Epub 2014 Dec 6.

Discovery and SAR study of 2-(4-pyridylamino)thieno[3,2-d]pyrimidin-4(3H)-ones as soluble and highly potent PDE7 inhibitors.

Author information

1
Drug Research Center, Kaken Pharmaceutical Co. Ltd, 14, Shinomiya Minamigawara-cho, Yamashina, Kyoto 607-8042, Japan.

Abstract

The discovery and SAR study of a new series of soluble and highly potent phosphodiesterase (PDE) 7 inhibitors are described herein. We explored a new lead compound with improved solubility, which led to the discovery of a 2-(4-pyridylamino)thieno[3,2-d]pyrimidin-4(3H)-one series. The introduction of 3-piperidines at the 7-position resulted in the significant enhancement of PDE7 activity. In particular, compound 32 also showed strong PDE7 inhibitory activity; good selectivity against PDE3, 4, and 5; and good aqueous solubility.

KEYWORDS:

Aqueous solubility; Phosphodiesterase; T-cell; Thienopyrimidinone

PMID:
25529739
DOI:
10.1016/j.bmcl.2014.11.090
[Indexed for MEDLINE]

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