Literature DB >> 17482819

Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.

William A Carroll1, Douglas M Kalvin, Arturo Perez Medrano, Alan S Florjancic, Ying Wang, Diana L Donnelly-Roberts, Marian T Namovic, George Grayson, Prisca Honoré, Michael F Jarvis.   

Abstract

Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X(7) antagonists were identified with similar potency to the lead compound 4 but with improved physiochemical properties. Compound 12 was active in a rat model of neuropathic pain.

Entities:  

Mesh：

Substances：

Year:  2007        PMID： 17482819     DOI： 10.1016/j.bmcl.2007.04.075

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


  6 in total

1.  P2X(7) Receptors in Neurological and Cardiovascular Disorders.

Authors:  Stephen D Skaper; Patrizia Debetto; Pietro Giusti
Journal:  Cardiovasc Psychiatry Neurol       Date:  2009-06-24

2.  Discovery of Fused Triazolo-thiadiazoles as Inhibitors of TNF-alpha: Pharmacophore Hybridization for Treatment of Neuropathic Pain.

Authors:  Monika Sharma; Vanamala Deekshith; Arvind Semwal; Dharmarajan Sriram; Perumal Yogeeswari
Journal:  Pain Ther       Date:  2012-09-11

3.  Cloning and pharmacological characterization of the dog P2X7 receptor.

Authors:  S Roman; F S Cusdin; E Fonfria; J A Goodwin; J Reeves; S C Lappin; L Chambers; D S Walter; W C Clay; A D Michel
Journal:  Br J Pharmacol       Date:  2009-10-08       Impact factor: 8.739

4.  Palladium-catalyzed highly regioselective mono and double Sonogashira cross-coupling reactions of 5-substituted-1,2,3-triiodobenzene under ambient conditions.

Authors:  Raed M Al-Zoubi; Mothana K Al-Omari; Walid K Al-Jammal; Michael J Ferguson
Journal:  RSC Adv       Date:  2020-04-24       Impact factor: 3.361

Review 5.  The P2X7 Receptor in Inflammatory Diseases: Angel or Demon?

Authors:  Luiz E B Savio; Paola de Andrade Mello; Cleide Gonçalves da Silva; Robson Coutinho-Silva
Journal:  Front Pharmacol       Date:  2018-02-06       Impact factor: 5.810

6.  Selective P2X(7) receptor antagonists for chronic inflammation and pain.

Authors:  William A Carroll; Diana Donnelly-Roberts; Michael F Jarvis
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.