Literature DB >> 16782335

Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.

István Borza1, Sándor Kolok, Anikó Gere, József Nagy, László Fodor, Kornél Galgóczy, József Fetter, Ferenc Bertha, Béla Agai, Csilla Horváth, Sándor Farkas, György Domány.   

Abstract

A novel series of benzimidazole-2-carboxamide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The influence of some structural elements, like H-bond donor groups placed on the benzimidazole skeleton and the substitution pattern of the piperidine ring, on the biological activity was studied. Compound 6a showed excellent analgetic activity in the mouse formalin test following po administration.

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Year:  2006        PMID: 16782335     DOI: 10.1016/j.bmcl.2006.06.002

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


  3 in total

Review 1.  Glutamate receptor ion channels: structure, regulation, and function.

Authors:  Stephen F Traynelis; Lonnie P Wollmuth; Chris J McBain; Frank S Menniti; Katie M Vance; Kevin K Ogden; Kasper B Hansen; Hongjie Yuan; Scott J Myers; Ray Dingledine
Journal:  Pharmacol Rev       Date:  2010-09       Impact factor: 25.468

Review 2.  Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential.

Authors:  Laetitia Mony; James N C Kew; Martin J Gunthorpe; Pierre Paoletti
Journal:  Br J Pharmacol       Date:  2009-07-08       Impact factor: 8.739

3.  Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity.

Authors:  Dmitry S Karlov; Nadezhda S Temnyakova; Dmitry A Vasilenko; Oleg I Barygin; Mikhail Y Dron; Arseniy S Zhigulin; Elena B Averina; Yuri K Grishin; Vladimir V Grigoriev; Alexey V Gabrel'yan; Viktor A Aniol; Natalia V Gulyaeva; Sergey V Osipenko; Yury I Kostyukevich; Vladimir A Palyulin; Petr A Popov; Maxim V Fedorov
Journal:  RSC Med Chem       Date:  2022-06-22
  3 in total

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