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Tunable regulatory activities of 1,10-phenanthroline derivatives towards acid sphingomyelinase and Zn(ii)–amyloid-β

Author:
YiThese authors contributed equally to this work., Yelim, Han, Jiyeon, Park, Min Hee, Park, Nahye, Nam, Eunju, Jin, Hee Kyung, Bae, Jae-sung, Lim, Mi Hee
Source:
Chemical communications 2019 v.55 no.42 pp. 5847-5850
ISSN:
1364-548X
Subject:
Alzheimer disease, binding capacity, brain, chemical reactions, enzymes, hydrophobicity, zinc
Abstract:
We report a new series of small molecules able to achieve the tunability of modulatory activities against acid sphingomyelinase (ASM) and Zn(ii)-bound amyloid-β [Zn(ii)–Aβ], two pathological targets found in the brain affected by Alzheimer's disease. Rational tuning of the hydrophobicity and Zn(ii) binding affinity of the 1,10-phenanthroline (phen) framework successfully yielded compounds as chemical modulators for ASM (4 and 5), Zn(ii)–Aβ (phen, 1, and 2), or both (3).
Agid:
6448025