Synthesis and evaluation of oxime derivatives as modulators for amyloid beta-induced mitochondrial dysfunction

Title
Synthesis and evaluation of oxime derivatives as modulators for amyloid beta-induced mitochondrial dysfunction
Authors
김영습정선화박병건고민경장현서최기항백자현이지연이재균배애님조용서민선준
Keywords
Alzheimer’s disease; Mitochondrial permeability transition pore (mPTP); Oxime derivatives; Amyloid beta; Pharmacokinetics
Issue Date
2013-04
Publisher
European journal of medicinal chemistry
Citation
VOL 62, 71-83
Abstract
Starting from quinuclidinyl oxime 1 identified by preliminary screening, a series of azacycles-containing oxime derivatives was synthesized. Their mPTP blocking activities were evaluated by a JC-1 assay, measuring the change of mitochondrial membrane potential. The inhibitory activity of nine compounds against amyloid beta-induced mPTP opening was comparable or even superior to that of piracetam. Among them, 12d effectively maintained mitochondrial function and cell viabilities on the ATP assay, the MTT assay, and the ROS assay. In addition, it exhibited favorable in vitro stability and pharmacokinetic characteristics, which hold a promise for further development of AD therapeutics.
URI
http://pubs.kist.re.kr/handle/201004/46171
ISSN
02235234
Appears in Collections:
KIST Publication > Article
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