Design, Synthesis, and Evaluation of a Novel 4-Aminomethyl-4-fluoropiperidine as a T-Type Ca2+Channel Antagonist
Journal of Medicinal Chemistry2008Vol. 51(13), pp. 3692–3695
Citations Over TimeTop 10% of 2008 papers
William D. Shipe, James C. Barrow, Zhi-Qiang Yang, Craig W. Lindsley, Fanglong Yang, Kelly-Ann S. Schlegel, Youheng Shu, Kenneth E. Rittle, Mark G. Bock, George D. Hartman, Cuyue Tang, Jeanine Ballard, Yuhsin Kuo, Emily D. Adarayan, Thomayant Prueksaritanont, Matthew M. Zrada, Victor N. Uebele, Cindy E. Nuss, Thomas 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
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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