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Bioorg Med Chem Lett. 2011 Dec 15;21(24):7287-90. doi: 10.1016/j.bmcl.2011.10.037. Epub 2011 Oct 21.

Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 2.

Author information

1
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA. Stephanie.Brumfield@merck.com

Abstract

Novel P2X(7) antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X(7) receptor in human and rodent as well as efficacious in rodent pain models. Compound 15a was identified to have oral potency in several pain models in rodent similar to naproxen, gabapentin and pregabalin. Structure-activity relationship (SAR) development and results of pain models are presented.

PMID:
22078214
DOI:
10.1016/j.bmcl.2011.10.037
[Indexed for MEDLINE]

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