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
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. [email protected]
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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