Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists
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- 作者：Helen E. Armstrong ; Amy Galka ; Linus S. Lin ; Jr. ; Thomas J. Lanza ; James P. Jewell ; Shrenik K. Shah ; Ravi Guthikonda ; Quang Truong ; Linda L. Chang ; Grace Quaker ; et al.
- 关键词：Cannabinoid ; CB-1R ; Sulfonamide ; Obesity
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：15 April 2007
- 年：2007
- 卷：17
- 期：8
- 页码：2184-2187
- 全文大小：239 K
文摘
Sulfonamide analogues of the potent CB1R inverse agonist taranabant were prepared and optimized for potency and selectivity for CB1R. They were variably more potent than the corresponding amide analogues. The most potent representative 22 had good pharmacokinetic and brain levels, but was modestly active in blocking CB1R agonist-mediated hypothermia.