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. Epub 2011 Jan 26.

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.

MeSH terms

  • Amides / pharmacology*
  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, T-Type / drug effects*
  • Mice
  • Rats
  • Rats, Wistar

Substances

  • Amides
  • Calcium Channel Blockers
  • Calcium Channels, T-Type