Abstract
The synthesis and structure-activity relationship (SAR) of a novel series of 3-(imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers, derived from a high throughput screening (HTS), are described. Subsequent optimization led to identification of potent, metabolically stable and orally available mGluR2 positive allosteric modulators (PAMs).
MeSH terms
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Administration, Oral
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Allosteric Regulation*
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Allosteric Site
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Animals
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Azabicyclo Compounds / chemical synthesis*
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Azabicyclo Compounds / pharmacology
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / pharmacology
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Drug Evaluation, Preclinical
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Ethers / chemistry*
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Humans
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Microsomes / drug effects
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Models, Chemical
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Rats
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Receptors, Metabotropic Glutamate / chemistry*
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Schizophrenia / drug therapy
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Structure-Activity Relationship
Substances
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Azabicyclo Compounds
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Benzimidazoles
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Ethers
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor 2