Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant

[摘要]：The design, synthesis, and binding activity of ring constrained analogs of the acyclic cannabinoid-1 receptor (CB1R) inverse agonist taranabant 1 are described. The initial inspiration for these taranabant derivatives was its conformation 1a, determined by H-1 NMR, X-ray, and molecular modeling. The constrained analogs were all much less potent than their acyclic parent structure. The results obtained are discussed in the context of a predicted binding of 1 to a homology model of CB1R. (C) 2010 Elsevier Ltd. All rights reserved.

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