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Bioorg Med Chem Lett. 2010 Aug 15;20(16):4757-61. doi: 10.1016/j.bmcl.2010.06.127. Epub 2010 Jul 1.

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

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.

Abstract

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 (1)H 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.

PMID:
20643546
DOI:
10.1016/j.bmcl.2010.06.127
[Indexed for MEDLINE]

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