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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
chemistry
Novel quinazoline-urea analogues as modulators for Aβ-induced mitochondrial dysfunction: Design, synthesis, and molecular docking study
European Journal of Medicinal Chemistry, Volume 84, Year 2014
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Description
A novel series of twenty-six quinazoline-urea derivatives was designed and synthesized. Their blocking activities against β-amyloid peptide (Aβ) induced mitochondrial permeability transition pore (mPTP) opening were evaluated by JC-1 assay which measured the change of mitochondrial membrane potential. Seven compounds showed better inhibitory activities than the standard Cyclosporin A (CsA). The most active analogues were tested by MTT assay to evaluate their toxicity on the cellular survival; they revealed excellent cellular viability. To explain the difference in inhibitory activity, molecular docking study using (GOLD) program was performed for selected sets of the most active and inactive compounds on cyclophilin D (CypD) receptor as a major component of mPTP. Moreover, ADME profiling, in silico toxicity, drug-likeness, and drug-score studies were discussed. From these results, we report compound 31 as the most active nonpeptidyl mPTP blocker possessing quinazoline-urea scaffold; 2 folds of CsA activity, which would constitute a new direction for the design of novel mPTP modulators. © 2014 Published by Elsevier Masson SAS.
Authors & Co-Authors
Elkamhawy, Ahmed
South Korea, Seoul
Korea Institute of Science and Technology
South Korea, Daejeon
University of Science and Technology Ust
Lee, Jiyoun
South Korea, Seoul
Sungshin Women's University
Park, Beoung-geon
South Korea, Seoul
Korea University
South Korea, Seoul
Korea Institute of Science and Technology
Pae, Aenim
South Korea, Seoul
Korea Institute of Science and Technology
Roh, Eunjoo
South Korea, Seoul
Korea Institute of Science and Technology
South Korea, Daejeon
University of Science and Technology Ust
Statistics
Citations: 33
Authors: 5
Affiliations: 5
Identifiers
Doi:
10.1016/j.ejmech.2014.07.027
ISSN:
02235234