Abstract
A novel class of (5-(pent-1-enyl)thiophen-2-yl)pyrazole antagonists was discovered, many of which exhibited potent CB1 activity and good CB1/2 selectivity, suggesting that along with a 1,3-transposition of the carbonyl of the pyrazole 3-carboxamide, bioisosteric replacement of the conventional pyrazole 5-aryl group with a thienyl ring substituted with an appropriate alkenyl moiety is viable.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Drug Design*
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Humans
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Inhibitory Concentration 50
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Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
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Receptor, Cannabinoid, CB1 / metabolism
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Receptor, Cannabinoid, CB2 / antagonists & inhibitors
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Receptor, Cannabinoid, CB2 / metabolism
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Substrate Specificity
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Thiophenes / chemical synthesis*
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Thiophenes / chemistry
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Thiophenes / metabolism
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Thiophenes / pharmacology*
Substances
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Receptor, Cannabinoid, CB1
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Receptor, Cannabinoid, CB2
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Thiophenes