Abstract
The triaryl bis-sulfone 1 was modified by converting the aryl A-ring to a piperidine ring. The piperidine ring was further elaborated to a spirocyclopropyl piperidine moiety. The effect on CB2 binding potency, rat calcium channel affinity, and CYP 2C9 inhibition is described.
Copyright 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Calcium Channels / metabolism
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Cytochrome P-450 Enzyme System
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Drug Inverse Agonism
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Humans
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Piperidines / chemistry
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Rats
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Receptor, Cannabinoid, CB2 / antagonists & inhibitors*
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Receptor, Cannabinoid, CB2 / metabolism
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacokinetics
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Sulfones / chemical synthesis*
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Sulfones / chemistry*
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Sulfones / pharmacokinetics
Substances
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Calcium Channels
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Piperidines
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Receptor, Cannabinoid, CB2
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Sulfonamides
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Sulfones
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piperidine
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Cytochrome P-450 Enzyme System