Discovery of triazines as potent, selective and orally active PDE4 inhibitors
Copyright policy )Discovery of triazines as potent, selective and orally active PDE4 inhibitors
Expanding on HTS hit 4 afforded a series of [1,3,5]triazine derivatives as novel PDE4 inhibitors. The SAR development and optimization process with the emphasis on ligand efficiency and physicochemical properties led to the discovery of compound 44 as a potent, selective and orally active PDE4 inhibitor.
Binding Sites, Cyclic Nucleotide Phosphodiesterases, Type 7, Triazines, Drug Evaluation, Preclinical, Administration, Oral, Cyclic Nucleotide Phosphodiesterases, Type 4, Protein Structure, Tertiary, Rats, Molecular Docking Simulation, Structure-Activity Relationship, Microsomes, Liver, Animals, Phosphodiesterase 4 Inhibitors, Half-Life
Binding Sites, Cyclic Nucleotide Phosphodiesterases, Type 7, Triazines, Drug Evaluation, Preclinical, Administration, Oral, Cyclic Nucleotide Phosphodiesterases, Type 4, Protein Structure, Tertiary, Rats, Molecular Docking Simulation, Structure-Activity Relationship, Microsomes, Liver, Animals, Phosphodiesterase 4 Inhibitors, Half-Life
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