Discovery of oxazole-based PDE4 inhibitors with picomolar potency.

Bioorganic & Medicinal Chemistry Letters(2012)

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摘要
Optimization of oxazole-based PDE4 inhibitors has led to the discovery of a series of quinolyl oxazoles, with 4-benzylcarboxamide and 5-α-aminoethyl groups which exhibit picomolar potency against PDE4. Selectivity profiles and in vivo biological activity are also reported.
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关键词
PDE4 inhibitor,Phosphodiesterase 4,Oxazole,Picomolar,Inflammation
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