Discovery of oral and inhaled PDE4 inhibitors.
| Autor: | Ting PC; Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA. Electronic address: pauline.ting@merck.com., Lee JF, Kuang R, Cao J, Gu D, Huang Y, Liu Z, Aslanian RG, Feng KI, Prelusky D, Lamca J, House A, Phillips JE, Wang P, Wu P, Lundell D, Chapman RW, Celly CS |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Oct 15; Vol. 23 (20), pp. 5528-32. Date of Electronic Publication: 2013 Aug 21. |
| DOI: | 10.1016/j.bmcl.2013.08.056 |
| Abstrakt: | 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.) |
| Databáze: | MEDLINE |
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