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Bioorg Med Chem. 2009 Apr 1;17(7):2842-51. doi: 10.1016/j.bmc.2009.02.027. Epub 2009 Feb 21.

Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists.

Author information

1
PharmaCenter Bonn, University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D-53121 Bonn, Germany.

Abstract

In the present study we synthesized 36 coumarin and 2H-chromene derivatives applying a recently developed umpoled domino reaction using substituted salicylaldehyde and alpha,beta-unsaturated aldehyde derivatives as starting compounds. In radioligand binding studies 5-substituted 3-benzylcoumarin derivatives showed affinity to cannabinoid CB(1) and CB(2) receptors and were identified as new lead structures. In further GTPgammaS binding studies selected compounds were shown to be antagonists or inverse agonists.

PMID:
19278853
DOI:
10.1016/j.bmc.2009.02.027
[Indexed for MEDLINE]

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