Literature DB >> 21570840

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

Julius J Matasi1, Stephanie Brumfield, Deen Tulshian, Michael Czarnecki, William Greenlee, Charles G Garlisi, Hongchen Qiu, Kristine Devito, Shu-Cheng Chen, Youngliang Sun, Rosalia Bertorelli, William Geiss, Van-Duc Le, Gregory S Martin, Samuel A Vellekoop, James Haber, Melissa L Allard.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21570840     DOI： 10.1016/j.bmcl.2011.04.034

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  Small Molecules in the Cone Snail Arsenal.

Authors:  Jorge L B Neves; Zhenjian Lin; Julita S Imperial; Agostinho Antunes; Vitor Vasconcelos; Baldomero M Olivera; Eric W Schmidt
Journal:  Org Lett       Date:  2015-09-30       Impact factor: 6.005

2.  Astrocytic CX43 hemichannels and gap junctions play a crucial role in development of chronic neuropathic pain following spinal cord injury.

Authors:  Michael J Chen; Benjamin Kress; Xiaoning Han; Katherine Moll; Weiguo Peng; Ru-Rong Ji; Maiken Nedergaard
Journal:  Glia       Date:  2012-08-01       Impact factor: 7.452

3.  Quantitative structure-activity relationship study of P2X7 receptor inhibitors using combination of principal component analysis and artificial intelligence methods.

Authors:  Mehdi Ahmadi; Mohsen Shahlaei
Journal:  Res Pharm Sci       Date:  2015 Jul-Aug
  3 in total

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