Abstract
A series of libraries were designed using the 1-(cyclopropylmethyl)-2-alkyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-5-ium templates 2a-b, and Sulfonamide derivatives 11a-n proved to be potent agonists of the CB(2) receptor. Analysis of the Lipophilic Efficiency (LipE) of potent compounds provided new insight for the design of potent, metabolically stable CB2 agonists.
MeSH terms
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Animals
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Binding Sites
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Chemistry, Pharmaceutical / methods
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Combinatorial Chemistry Techniques
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Drug Design
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Inhibitory Concentration 50
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Ligands
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Microsomes, Liver / drug effects
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Models, Chemical
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Molecular Structure
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Nitrogen / chemistry
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Rats
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Receptor, Cannabinoid, CB2 / chemistry*
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Structure-Activity Relationship
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Sulfonamides / chemistry
Substances
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Ligands
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Receptor, Cannabinoid, CB2
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Sulfonamides
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Nitrogen