Abstract
A series of phenylimidazole-pyrazolo[1,5-c]quinazolines 1a-q was designed, synthesized and characterised as a novel class of potent phophodiesterase 10A (PDE10A) inhibitors. In this series, 2,9-dimethyl-5-(2-(1-methyl-4-phenyl-1H-imidazol-2-yl)ethyl)pyrazolo[1,5-c]quinazoline (1q) showed the highest affinity for PDE10A enzyme (IC(50)=16nM).
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MeSH terms
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Animals
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Blood-Brain Barrier
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Inhibitory Concentration 50
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Mice
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Models, Molecular
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Phosphodiesterase Inhibitors / chemical synthesis*
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Phosphodiesterase Inhibitors / chemistry
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Phosphodiesterase Inhibitors / pharmacology*
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Phosphoric Diester Hydrolases / drug effects*
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Quinazolines / chemical synthesis*
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Quinazolines / chemistry
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Quinazolines / pharmacology*
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Structure-Activity Relationship
Substances
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Phosphodiesterase Inhibitors
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Quinazolines
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Pde10a protein, mouse
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Phosphoric Diester Hydrolases