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

Title
Discovery of benzimidazole derivatives as modulators of mitochondrial function: A potential treatment for Alzheimer's disease
Author
민선준
Keywords
Translocator protein; TSPO; Mitochondrial permeability transition pore; Alzheimer's disease; Mitochondrial dysfunction; A beta; PERMEABILITY TRANSITION PORE; AMYLOID-BETA; CYCLOSPORINE-A; CYCLOPHILIN-D; BRAIN-INJURY; MOUSE MODEL; DYSFUNCTION; INHIBITOR; TSPO; REPERFUSION
Issue Date
2017-01
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 125, Page. 1172-1192
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 A beta-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. (C) 2016 Elsevier Masson SAS. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S0223523416309552http://repository.hanyang.ac.kr/handle/20.500.11754/71621
ISSN
0223-5234; 1768-3254
DOI
10.1016/j.ejmech.2016.11.017
Appears in Collections:
COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E](과학기술융합대학) > CHEMICAL AND MOLECULAR ENGINEERING(화학분자공학과) > Articles
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