Abstract
Structure-activity relationship studies focused on bio-isosteric replacements of 2-pyridyl resulted in mGlu5 receptor antagonists with reduced inhibition of cytochrome P450 1A2. This led to highly potent, selective and orally bioavailable 2-imidazolyl tetrazoles such as (10) that are devoid of cytochrome P450 inhibitory activity.
MeSH terms
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Administration, Oral
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Animals
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Anti-Anxiety Agents / chemical synthesis
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Anti-Anxiety Agents / chemistry
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Anti-Anxiety Agents / pharmacokinetics
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Biological Availability
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Cytochrome P-450 CYP1A2 Inhibitors*
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Molecular Structure
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Rats
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Rats, Sprague-Dawley
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Receptor, Metabotropic Glutamate 5
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Receptors, Metabotropic Glutamate / antagonists & inhibitors*
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Structure-Activity Relationship
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Tetrazoles / chemical synthesis*
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Tetrazoles / chemistry
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Tetrazoles / pharmacokinetics*
Substances
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Anti-Anxiety Agents
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Cytochrome P-450 CYP1A2 Inhibitors
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Receptor, Metabotropic Glutamate 5
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Receptors, Metabotropic Glutamate
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Tetrazoles