Abstract
Benzimidazolone derivatives were discovered as novel CB2 selective agonists. Structure Activity Relationship (SAR) studies around them were examined to improve metabolic stability. Compound 39 exhibited excellent metabolic stability in human liver microsomes (HLM) and significant attenuation of the chronic colonic allodynia in the TNBS-treated rats by po administration.
MeSH terms
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Animals
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology*
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Combinatorial Chemistry Techniques
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Drug Design
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Humans
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Molecular Structure
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Rats
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Receptor, Cannabinoid, CB1 / agonists
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Receptor, Cannabinoid, CB2 / agonists*
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Structure-Activity Relationship
Substances
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Benzimidazoles
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Receptor, Cannabinoid, CB1
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Receptor, Cannabinoid, CB2
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benzimidazolone