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

✍ Scribed by Ihor E. Kopka; Linus S. Lin; James P. Jewell; Thomas J. Lanza; Tung M. Fong; Chun-Pyn Shen; Zhege J. Lao; Sookhee Ha; Laurie G. Castonguay; Lex Van der Ploeg; Mark T. Goulet; William K. Hagmann

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 1000 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.06.127

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✦ Synopsis

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.

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