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

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          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.

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          Author and article information

          Journal
          Bioorg. Med. Chem.
          Bioorganic & medicinal chemistry
          Elsevier BV
          1464-3391
          0968-0896
          Apr 01 2009
          : 17
          : 7
          Affiliations
          [1 ] PharmaCenter Bonn, University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D-53121 Bonn, Germany.
          Article
          S0968-0896(09)00182-5
          10.1016/j.bmc.2009.02.027
          19278853
          1ad02402-1153-4a4e-af00-0f755c7bccd3
          History

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