Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371322 | Bioorganic & Medicinal Chemistry Letters | 2015 | 5 Pages |
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.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Yusuke Endo, Kentaro Kawai, Takeshi Asano, Seiji Amano, Yoshihito Asanuma, Keisuke Sawada, Keiji Ogura, Naoya Nagata, Noriko Ueo, Nobuaki Takahashi, Yo Sonoda, Noriyuki Kamei,