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

Tae Hun Kim, Ha Yun Yang, Beoung Gun Park, Seo Yun Jung, Jong Hyun Park, Ki Duk Park, Sun Joon Min, Jinsung Tae, Hyejin Yang, Suengmok Cho, Sung Jin Cho, Hyundong Song, Inhee Mook-Jung, Jiyoun Lee, Ae Nim Pae

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16 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1172-1192
Number of pages21
JournalEuropean Journal of Medicinal Chemistry
Volume125
DOIs
Publication statusPublished - 2017 Jan 1

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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    Kim, T. H., Yang, H. Y., Park, B. G., Jung, S. Y., Park, J. H., Park, K. D., Min, S. J., Tae, J., Yang, H., Cho, S., Cho, S. J., Song, H., Mook-Jung, I., Lee, J., & Pae, A. N. (2017). Discovery of benzimidazole derivatives as modulators of mitochondrial function: A potential treatment for Alzheimer's disease. European Journal of Medicinal Chemistry, 125, 1172-1192. https://doi.org/10.1016/j.ejmech.2016.11.017