Kim, Young Seub Jung, Sun Hwa Park, Beoung-Geon Ko, Min Kyung Jang, Hyun-Seo Choi, Kihang Baik, Ja-Hyun Lee, Jiyoun Lee, Jae Kyun Pae, Ae Nim Cho, Yong Seo Min, Sun-Joon 2024-01-20T12:33:36Z 2024-01-20T12:33:36Z 2021-09-05 2013-04 0223-5234 https://pubs.kist.re.kr/handle/201004/128207 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. (C) 2012 Elsevier Masson SAS. All rights reserved. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER PERMEABILITY TRANSITION ALZHEIMERS-DISEASE DIMEBON TRANSPORT ENHANCER Synthesis and evaluation of oxime derivatives as modulators for amyloid beta-induced mitochondrial dysfunction Article 10.1016/j.ejmech.2012.12.033 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.62, pp.71 - 83 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 62 71 83 scie scopus 000318577500008 2-s2.0-84872676241 Chemistry, Medicinal Pharmacology & Pharmacy Article PERMEABILITY TRANSITION ALZHEIMERS-DISEASE DIMEBON TRANSPORT ENHANCER Alzheimer&apos s disease Mitochondrial permeability transition pore (mPTP) Oxime derivatives Amyloid beta Pharmacokinetics