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J Med Chem. 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.

Author information

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

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.

PMID:
18540666
DOI:
10.1021/jm800419w
[Indexed for MEDLINE]
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