Discovery of oxazole-based PDE4 inhibitors with picomolar potency
Copyright policy )Discovery of oxazole-based PDE4 inhibitors with picomolar potency
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.
- Merck & Co. United States
Models, Molecular, Tumor Necrosis Factor-alpha, Anti-Inflammatory Agents, Cyclic Nucleotide Phosphodiesterases, Type 4, Rats, Cyclic N-Oxides, Structure-Activity Relationship, Drug Discovery, Quinolines, Animals, Humans, Phosphodiesterase 4 Inhibitors, Oxazoles
Models, Molecular, Tumor Necrosis Factor-alpha, Anti-Inflammatory Agents, Cyclic Nucleotide Phosphodiesterases, Type 4, Rats, Cyclic N-Oxides, Structure-Activity Relationship, Drug Discovery, Quinolines, Animals, Humans, Phosphodiesterase 4 Inhibitors, Oxazoles
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