Design, synthesis, and evaluation of a novel 4-aminomethyl-4- fluoropiperidine as a T-type Ca2+ channel antagonist

William D. Shipe, James C. Barrow, Zhi Qiang Yang, Craig W. Lindsley, F. Vivien Yang, Kelly Ann S. Schlegel, Youheng Shu, Kenneth E. Rittle, Mark G. Bock, George D. Hartman, Cuyue Tang, Jeanine E. Ballard, Yuhsin Kuo, Emily D. Adarayan, Thomayant Prueksaritanont, Matthew M. Zrada, Victor N. Uebele, Cindy E. Nuss, Thomas M. Connolly, Scott M. DoranSteven V. Fox, Richard L. Kraus, Michael J. Marino, Valerie Kuzmick Graufelds, Hugo M. Vargas, Patricia B. Bunting, Martha Hasbun-Manning, Rose M. Evans, Kenneth S. Koblan, John J. Renger

Research output: Contribution to journalArticlepeer-review

Abstract

The novel T-type antagonist (S)-5 has been prepared and evaluated in in vitro and in vivo assays for T-type calcium ion channel activity. Structural modification of the piperidine leads 1 and 2 afforded the fluorinated piperidine (S)-5, a potent and selective antagonist that displayed in vivo CNS efficacy without adverse cardiovascular effects.

Original languageEnglish (US)
Pages (from-to)3692-3695
Number of pages4
JournalJournal of medicinal chemistry
Volume51
Issue number13
DOIs
StatePublished - Jul 10 2008
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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