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.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Amyloid beta (Aβ or Abeta) is a peptide of 36–43 amino acids that is processed from the Amyloid precursor protein. While best known as a component of amyloid plaques in association with Alzheimer's disease, evidence has been found that Aβ is a highly multifunctional peptide with significant non-pathological activity.[1] Aβ is the main component of deposits found in the brains of patients with Alzheimer's disease
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The secret of Eta Black by Ananya Sharma
The secret of Eta Black by Ananya Sharma A man sitting behind the bars named Eta black has no clue what is happening with him. He was searc...
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