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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Matasi JJ,Brumfield S,Tulshian D,Czarnecki M,Greenlee W,Garlisi CG,Qiu H,Devito K,Chen SC,Sun Y,Bertorelli R,Geiss W,Le VD,Martin GS,Vellekoop SA,Haber J,Allard ML

doi

10.1016/j.bmcl.2011.04.034

subject

Has Abstract

pub_date

2011-06-15 00:00:00

pages

3805-8

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00490-2

journal_volume

21

pub_type

杂志文章

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