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. 2008 Jul 10;51(13):3692-5.
doi: 10.1021/jm800419w. Epub 2008 Jun 10.

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

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

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

William D Shipe et al. J Med Chem. .

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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