Literature DB >> 25113934

Discovery of pyrrolo-benzo-1,4-diazines as potent Na(v)1.7 sodium channel blockers.

Ginny D Ho1, Deen Tulshian1, Ana Bercovici1, Zheng Tan1, Jennifer Hanisak1, Stephanie Brumfield1, Julius Matasi1, Charles R Heap2, William G Earley2, Brandy Courneya2, R Jason Herr2, Xiaoping Zhou3, Terry Bridal4, Diane Rindgen5, Steve Sorota4, Shu-Wei Yang6.   

Abstract

A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described. Compound 41 displayed anti-nociceptive efficacy in the rat CFA pain model at 100 mpk oral dosing.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Nav1.5; Nav1.7; Pain; Pyrrolo-benzo-1,4-diazine; Sodium channel blockers

Mesh：

Substances：

Year:  2014        PMID： 25113934     DOI： 10.1016/j.bmcl.2014.07.060

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


  3 in total

Review 1.  Inhibition of NaV1.7: the possibility of ideal analgesics.

Authors:  Yutaka Kitano; Tsuyoshi Shinozuka
Journal:  RSC Med Chem       Date:  2022-08-01

2.  Chemical Synthesis, Proper Folding, Nav Channel Selectivity Profile and Analgesic Properties of the Spider Peptide Phlotoxin 1.

Authors:  Sébastien Nicolas; Claude Zoukimian; Frank Bosmans; Jérôme Montnach; Sylvie Diochot; Eva Cuypers; Stephan De Waard; Rémy Béroud; Dietrich Mebs; David Craik; Didier Boturyn; Michel Lazdunski; Jan Tytgat; Michel De Waard
Journal:  Toxins (Basel)       Date:  2019-06-21       Impact factor: 4.546

3.  Tin(ii) chloride dihydrate/choline chloride deep eutectic solvent: redox properties in the fast synthesis of N-arylacetamides and indolo(pyrrolo)[1,2-a]quinoxalines.

Authors:  Sergio Alfonso Trujillo; Diana Peña-Solórzano; Oscar Rodríguez Bejarano; Cristian Ochoa-Puentes
Journal:  RSC Adv       Date:  2020-11-06       Impact factor: 3.361
  3 in total

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