Nesi_2017_Eur.J.Med.Chem_141_232

Reference

Title : Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease - Nesi_2017_Eur.J.Med.Chem_141_232
Author(s) : Nesi G , Chen Q , Sestito S , Digiacomo M , Yang X , Wang S , Pi R , Rapposelli S
Ref : Eur Journal of Medicinal Chemistry , 141 :232 , 2017
Abstract :

Starting from nature as original source, new potential agents with pleiotropic activities have been synthesized and evaluated as neuroprotective agents. In this work, novel nature-based hybrids, combining antioxidant motifs with rivastigmine, have been designed and synthesized. The biological results revealed that the new compounds inhibit both AChE and BuChE. In particular, lipoic acid hybrids LA1, LA2, LA3 resulted to be the most potent inhibitors of BuChE showing IC(50) values ranging from 340 to 378 nM. Analogously, all the compounds were able to inhibit the self beta-amyloid(1-42) aggregation. The gallic acid hybrid GA2 as well as the 2-chromonecarboxylic acid hybrids CA1 and CA2 prevented the self-mediated Abeta aggregation with percentages of inhibition ranging from 53% to 59%. Finally, some of them also show potent neuroprotective effects against glutamate-induced cell death and low toxicity in HT22 cells.

PubMedSearch : Nesi_2017_Eur.J.Med.Chem_141_232
PubMedID: 29031070

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Citations formats

Nesi G, Chen Q, Sestito S, Digiacomo M, Yang X, Wang S, Pi R, Rapposelli S (2017)
Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease
Eur Journal of Medicinal Chemistry 141 :232

Nesi G, Chen Q, Sestito S, Digiacomo M, Yang X, Wang S, Pi R, Rapposelli S (2017)
Eur Journal of Medicinal Chemistry 141 :232