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Bioorg Med Chem Lett. 2010 Aug 1;20(15):4602-6. doi: 10.1016/j.bmcl.2010.06.012. Epub 2010 Jun 8.

T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, USA. elizabeth.m.smith@spcorp.com

Abstract

A series of spiro-azetidines and azetidinones has been evaluated as novel blockers of the T-type calcium channel (Ca(V)3.2) which is a new therapeutic target for the potential treatment of both inflammatory and neuropathic pain. Confirmation and optimization of the potency, selectivity and DMPK properties of leads will be described.

PMID:
20580233
DOI:
10.1016/j.bmcl.2010.06.012
[Indexed for MEDLINE]

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