| Literature DB >> 17293109 |
Helen E Armstrong1, Amy Galka, Linus S Lin, Thomas J Lanza, James P Jewell, Shrenik K Shah, Ravi Guthikonda, Quang Truong, Linda L Chang, Grace Quaker, Vincent J Colandrea, Xinchun Tong, Junying Wang, Sherry Xu, Tung M Fong, Chun-Pyn Shen, Julie Lao, Jing Chen, Lauren P Shearman, D Sloan Stribling, Kimberly Rosko, Alison Strack, Sookhee Ha, Lex Van der Ploeg, Mark T Goulet, William K Hagmann.
Abstract
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.Entities:
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Year: 2007 PMID： 17293109 DOI： 10.1016/j.bmcl.2007.01.087
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823