Pyridyl amides as potent inhibitors of T-type calcium channels

Thomas S. Reger, 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. UebeleJohn J. Renger, James C. Barrow

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish (US)
Pages (from-to)1692-1696
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number6
DOIs
StatePublished - Mar 15 2011
Externally publishedYes

Keywords

  • Electrocorticogram
  • Epilepsy
  • Pregnane X receptor
  • Structure-activity relationships
  • T-type calcium channel

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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