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P1‐307: Inhibition of protein misfolding by optimization of small molecules targeted to both beta‐amyloid and tau peptides
Author(s) -
Taylor Marcia,
Banfield Scott,
Barden Christopher,
Lu Erhu,
Reed Mark,
Sweeting Braden,
Wang Yanfei,
Yadav Arun,
Yang Seung-Pil,
Weaver Donald F.,
Wu Fan
Publication year - 2015
Publication title -
alzheimer's and dementia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 6.713
H-Index - 118
eISSN - 1552-5279
pISSN - 1552-5260
DOI - 10.1016/j.jalz.2015.06.522
Subject(s) - amyloid (mycology) , chemistry , in vitro , amyloid beta , in silico , amyloid precursor protein , small molecule , surface plasmon resonance , biochemistry , pharmacology , peptide , biophysics , alzheimer's disease , medicine , biology , disease , pathology , gene , nanotechnology , materials science , inorganic chemistry , nanoparticle
with bromochloropropane to obtain an intermediate which was subsequently treated with various cyclic amines (1a-1f). Docking study of the compounds was performed using vlife 4.3 having crystal structure of TcAChE. Results: Docking study of the analogs revealed that they could bind to both the catalytic and peripheral sites as they interacts with various amino acid residues of the gorge like Trp279, Tyr121, Gly118, Gly119, Glu99 and Trp84. Conclusions:Coumarin analogues may alter the progression of disease as the analogs interact with both the sites of enzyme.