2. Academic Validation
  3. Pyridyl amides as potent inhibitors of T-type calcium channels

Pyridyl amides as potent inhibitors of T-type calcium channels

  • Bioorg Med Chem Lett. 2011 Mar 15;21(6):1692-6. doi: 10.1016/j.bmcl.2011.01.089.
Thomas S Reger 1,  Zhi-Qiang Yang,  Kelly-Ann S Schlegel,  Youheng Shu,  Christa Mattern,  Rowena Cube,  Kenneth E Rittle,  Georgia B McGaughey,  George D Hartman,  Cuyue Tang,  Jeanine Ballard,  Yuhsin Kuo,  Thomayant Prueksaritanont,  Cindy E Nuss,  Scott M Doran,  Steven V Fox,  Susan L Garson,  Yuxing Li,  Richard L Kraus,  Victor N Uebele,  John J Renger,  James C Barrow
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. thomas_reger@merck.com
PMID: 21316226 DOI: 10.1016/j.bmcl.2011.01.089
Abstract

A novel series of amide T-type calcium channel antagonists were prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 led to identification of the potent and selective T-type antagonist 37 that displayed in vivo efficacy in rodent models of epilepsy and sleep.

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