Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease

Article abstract of DOI:10.1016/j.ejmech.2016.04.069

An important part of pathogenesis of Alzheimer's disease (AD) is attributed to the contribution of AGE (Advanced Glycation Endproducts) and ALE (Advanced Lipid peroxidation Endproducts). In order to attenuate the progression of AD, we designed a new type of molecules that consist of two trapping parts for reactive carbonyl species (RCS) and reactive oxygen species (ROS), precursors of AGE and ALE, respectively. These molecules also chelate transition metals, the promoters of ROS formation. In this paper, synthesis of the new AGE/ALE inhibitors and evaluation of their physicochemical and biological properties (carbonyl trapping capacity, antioxidant activity, Cu²⁺-chelating capacity, cytotoxicity and protective effect against in?vitro MGO-induced apoptosis in the model AD cell-line PC12) are described. It is found that compounds 40b and 51e possess promising therapeutic potentials for treating AD.

Full text of DOI:10.1016/j.ejmech.2016.04.069

Accepted Manuscript
TEMPORARY REMOVAL: Multifunctional diamine AGE/ALE inhibitors with potential
therapeutical properties against Alzheimer’s disease
Elodie Lohou, N. André Sasaki, Agnès Boullier, Pascal Sonnet
PII:
S0223-5234(16)30362-2
10.1016/j.ejmech.2016.04.069
EJMECH 8584
DOI:
Reference:
To appear in: European Journal of Medicinal Chemistry
Please cite this article as: E. Lohou, N.A. Sasaki, A. Boullier, P. Sonnet, TEMPORARY REMOVAL:
Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer’s
disease, European Journal of Medicinal Chemistry (2016), doi: 10.1016/j.ejmech.2016.04.069.
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ACCEPTED MANUSCRIPT
TEMPORARY REMOVAL: Multifunctional diamine AGE/ALE inhibitors
with potential therapeutical properties against Alzheimer’s disease
a
a
Elodie Lohou , N. Andre Sasaki , Agnes Boullierb,c,d, Pascal Sonneta
ꢀ
ꢁ
a Universitꢀe de Picardie Jules Verne, Laboratoire de Glycochimie des Antimicrobiens et des Agroressouces,
LG2A, UMR CNRS 7378, UFR de Pharmacie, 1 Rue des Louvels, F-80037 Amiens Cedex 01, France
b Universitꢀe de Picardie Jules Verne, UFR de Mꢀedecine, 1 Rue des Louvels, F-80037 Amiens Cedex 01,
France
c INSERM U1088, Centre Universitaire de Recherche en Santꢀe (CURS), Avenue Renꢀe La€ennec - Salouel, F-
80054 Amiens Cedex 01, France
d CHU Amiens Picardie, Avenue Renꢀe La€ennec - Salouel, F-80054 Amiens Cedex 01, France
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