Abstract
Synthesis, in vitro biological evaluation, and structure-activity relationships of a biaryl cannabinoid mimetic 2 are reported. Variations in the substitution pattern yielded a number of agonists with low nanomolar affinity. Replacing the phenol group by a methyl morpholino acetate group led to compound 28, a 500-fold selective CB(2) receptor agonist.
MeSH terms
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Cannabinoids / chemical synthesis*
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Cannabinoids / chemistry*
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Carboxylic Acids / chemistry
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Drug Evaluation, Preclinical
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Humans
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Hydrogen / chemistry
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Hydrogen Bonding
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Immunosuppressive Agents / chemistry
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Inhibitory Concentration 50
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Kinetics
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Models, Chemical
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Parasympatholytics
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Phenol / chemistry
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Protein Binding
Substances
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Cannabinoids
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Carboxylic Acids
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Immunosuppressive Agents
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Parasympatholytics
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Phenol
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Hydrogen