Discovery of oral and inhaled PDE4 inhibitors

Discovery of oral and inhaled PDE4 inhibitors

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. The optimization of oxazole-based PDE4 inhibito...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2013-10, Vol.23 (20), p.5528-5532
Hauptverfasser: Ting, Pauline C., Lee, Joe F., Kuang, Rongze, Cao, Jianhua, Gu, Danlin, Huang, Ying, Liu, Zhidan, Aslanian, Robert G., Feng, Kung-I., Prelusky, Daniel, Lamca, James, House, Aileen, Phillips, Jonathan E., Wang, Peng, Wu, Ping, Lundell, Daniel, Chapman, Richard W., Celly, Chander S.
Format: Artikel
Sprache:eng
Schlagworte:
Administration, Oral
Animals
Asthma
COPD
Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry
Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism
Drug Evaluation, Preclinical
Half-Life
Inhalation
Oxazoles - chemical synthesis
Oxazoles - chemistry
Oxazoles - pharmacokinetics
PDE4 inhibitor
Phosphodiesterase 4 Inhibitors - chemical synthesis
Phosphodiesterase 4 Inhibitors - chemistry
Phosphodiesterase 4 Inhibitors - pharmacokinetics
Proline - analogs & derivatives
Proline - chemical synthesis
Proline - chemistry
Proline - pharmacokinetics
Quinolines - chemical synthesis
Quinolines - chemistry
Quinolines - pharmacokinetics
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
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Zusammenfassung: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.08.056