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Bioorg Med Chem Lett. 2010 Jan 15;20(2):608-11. doi: 10.1016/j.bmcl.2009.11.084. Epub 2009 Nov 22.

Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA. eric.gilbert@spcorp.com

Abstract

The triaryl bis-sulfone 1 was modified by converting the aryl A-ring to a piperidine ring. The piperidine ring was further elaborated to a spirocyclopropyl piperidine moiety. The effect on CB2 binding potency, rat calcium channel affinity, and CYP 2C9 inhibition is described.

PMID:
20005710
DOI:
10.1016/j.bmcl.2009.11.084
[Indexed for MEDLINE]

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