Abstract
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.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
-
Animals
-
Anti-Inflammatory Agents / chemical synthesis*
-
Anti-Inflammatory Agents / pharmacology
-
Cyclic N-Oxides / chemistry
-
Cyclic Nucleotide Phosphodiesterases, Type 4 / chemistry*
-
Cyclic Nucleotide Phosphodiesterases, Type 4 / metabolism
-
Drug Discovery
-
Humans
-
Models, Molecular
-
Oxazoles / chemical synthesis*
-
Oxazoles / pharmacology
-
Phosphodiesterase 4 Inhibitors / chemical synthesis*
-
Phosphodiesterase 4 Inhibitors / pharmacology
-
Quinolines / chemical synthesis*
-
Quinolines / chemistry
-
Quinolines / pharmacology
-
Rats
-
Structure-Activity Relationship
-
Tumor Necrosis Factor-alpha / antagonists & inhibitors
Substances
-
Anti-Inflammatory Agents
-
Cyclic N-Oxides
-
Oxazoles
-
Phosphodiesterase 4 Inhibitors
-
Quinolines
-
SCH 351591
-
Tumor Necrosis Factor-alpha
-
Cyclic Nucleotide Phosphodiesterases, Type 4