2. Academic Validation
  3. Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist

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

  • J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w.
William D Shipe 1,  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 Doran,  Steven 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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, WP14-1, P.O. Box 4, Sumneytown Pike, West Point, Pennsylvania 19486, USA. william_shipe@merck.com
PMID: 18540666 DOI: 10.1021/jm800419w
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.

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