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Bioorg Med Chem Lett. 2011 Jun 15;21(12):3805-8. doi: 10.1016/j.bmcl.2011.04.034. Epub 2011 Apr 24.

Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1.

Author information

1
Merck Research Laboratories, Kenilworth, NJ 07033-0539, USA. Julius.Matasi@merck.com

Abstract

Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X(7) receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and selective at the P2X(7) receptor in both human and rodent. Compound (entry 31) exhibited oral efficacy in the rat MIA and CCI pain models.

PMID:
21570840
DOI:
10.1016/j.bmcl.2011.04.034
[Indexed for MEDLINE]

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