Literature DB >> 27855359

Discovery of benzimidazole derivatives as modulators of mitochondrial function: A potential treatment for Alzheimer's disease.

TaeHun Kim1, Ha Yun Yang2, Beoung Gun Park3, Seo Yun Jung3, Jong-Hyun Park3, Ki Duk Park1, Sun-Joon Min4, Jinsung Tae5, Hyejin Yang6, Suengmok Cho6, Sung Jin Cho7, Hyundong Song8, Inhee Mook-Jung8, Jiyoun Lee9, Ae Nim Pae10.   

Abstract

In this study, we designed a library of compounds based on the structures of well-known ligands of the 18 kDa translocator protein (TSPO), one of the putative components of the mPTP. We performed diverse mitochondrial functional assays to assess their ability to restore cells from Aβ-induced toxicity in vitro and in vivo. Among tested compounds, compound 25 effectively improved cognitive function in animal models of AD. Given the excellent in vitro and in vivo activity and a favorable pharmacokinetic profile of compound 25, we believe that it can serve as a promising lead compound for a potential treatment option for AD. Copyright Â
© 2016 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Alzheimer's disease; Aβ; Mitochondrial dysfunction; Mitochondrial permeability transition pore; TSPO; Translocator protein

Mesh:

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Year:  2016        PMID: 27855359     DOI: 10.1016/j.ejmech.2016.11.017

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

1.  Synthesis, density functional theory study and in vitro antimicrobial evaluation of new benzimidazole Mannich bases.

Authors:  Maria Marinescu; Ludmila Otilia Cinteză; George Iuliu Marton; Mariana-Carmen Chifiriuc; Marcela Popa; Ioana Stănculescu; Christina-Marie Zălaru; Cristina-Elena Stavarache
Journal:  BMC Chem       Date:  2020-07-25

2.  Mitochondria modulatory effects of new TSPO ligands in a cellular model of tauopathies.

Authors:  Amandine Grimm; Imane Lejri; François Hallé; Martine Schmitt; Jürgen Götz; Frederic Bihel; Anne Eckert
Journal:  J Neuroendocrinol       Date:  2019-10-13       Impact factor: 3.627

3.  Mitochondrial dysfunction and Alzheimer's disease: prospects for therapeutic intervention.

Authors:  Ji Woong Lim; Jiyoun Lee; Ae Nim Pae
Journal:  BMB Rep       Date:  2020-01       Impact factor: 4.778

4.  TSPO Ligands Boost Mitochondrial Function and Pregnenolone Synthesis.

Authors:  Imane Lejri; Amandine Grimm; François Hallé; Mustapha Abarghaz; Christian Klein; Michel Maitre; Martine Schmitt; Jean-Jacques Bourguignon; Ayikoe Guy Mensah-Nyagan; Frederic Bihel; Anne Eckert
Journal:  J Alzheimers Dis       Date:  2019       Impact factor: 4.472

  4 in total

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