Caffeic acid phenethyl ester (CAPE)-derivatives act as selective inhibitors of acetylcholinesterase.

Basic Information

ID: ALA4393723

Journal: Eur J Med Chem

Title: Caffeic acid phenethyl ester (CAPE)-derivatives act as selective inhibitors of acetylcholinesterase.

Authors: Gießel JM, Loesche A, Csuk R, Serbian I.

Abstract: Unexpected inhibitory effects against eeAChE could be found for a newly synthesized class of caffeic acid phenethyl ester (CAPE) derivatives. Thus, phenethyl-(E)-3-(3,5-dimethoxy-4-phenethoxyphenyl)-acrylate (K_i = 1.97 ± 0.38 μM, K_i´ = 2.44 ± 0.07 μM) and 4-(2-(((E)-3-(3,4-bis(benzyloxy)phenyl)acryloyl)oxy)ethyl)-1,2-phenylene (2E,2'E)-bis(3-(3,4-bis(benzyloxy)phenyl)acrylate) (K_i = 0.72 ± 0.31 μM, K_i´ = 1.80 ± 0.21 μM) showed very good inhibition of eeAChE, while being non cytotoxic for malignant human cancer cells and non-malignant mouse fibroblasts. Also, they are weak inhibitors for BChE (from equine serum).

CiteXplore: 31158743

DOI: 10.1016/j.ejmech.2019.05.059

Patent ID: ┄

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