Highly potent PDE4 inhibitors with therapeutic potential

Based on the hypothesis that the dose-limiting side effects of PDE4 inhibitors could be mediated via the central nervous system (CNS), design and synthesis of a hydrophilic analogue is considered to be one approach to improving the side-effect profile of Ariflo™ 1. Water-soluble piperidine derivativ...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-01, Vol.14 (1), p.207-210
Main Authors: Ochiai, Hiroshi, Ohtani, Tazumi, Ishida, Akiharu, Kusumi, Kensuke, Kato, Masashi, Kohno, Hiroshi, Kishikawa, Katuya, Obata, Takaaki, Nakai, Hisao, Toda, Masaaki
Format: Article
Language:English
Subjects:
3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors
3',5'-Cyclic-AMP Phosphodiesterases - metabolism
Animals
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Bronchoconstriction - drug effects
Bronchoconstriction - physiology
Cyclic Nucleotide Phosphodiesterases, Type 4
Cyclohexanecarboxylic Acids - adverse effects
Cyclohexanecarboxylic Acids - chemistry
Gastric Emptying - drug effects
Gastric Emptying - physiology
Guinea Pigs
Humans
Medical sciences
Nitriles
Pharmacology. Drug treatments
Phosphodiesterase Inhibitors - chemistry
Phosphodiesterase Inhibitors - pharmacology
Phosphodiesterase Inhibitors - therapeutic use
Piperidines - chemistry
Piperidines - pharmacology
Rats
Respiratory system
Tumor Necrosis Factor-alpha - biosynthesis
U937 Cells
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Description
Summary:Based on the hypothesis that the dose-limiting side effects of PDE4 inhibitors could be mediated via the central nervous system (CNS), design and synthesis of a hydrophilic analogue is considered to be one approach to improving the side-effect profile of Ariflo™ 1. Water-soluble piperidine derivatives were found to possess therapeutic potential. Synthesis and biological evaluation of piperidine derivatives is reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.09.087