Synthesis and evaluation of oxime derivatives as modulators for amyloid beta-induced mitochondrial dysfunction
- Synthesis and evaluation of oxime derivatives as modulators for amyloid beta-induced mitochondrial dysfunction
- 김영습; 정선화; 박병건; 고민경; 장현서; 최기항; 백자현; 이지연; 이재균; 배애님; 조용서; 민선준
- Alzheimer’s disease; Mitochondrial permeability transition pore (mPTP); Oxime derivatives; Amyloid beta; Pharmacokinetics
- Issue Date
- European journal of medicinal chemistry
- VOL 62, 71-83
- 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.
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