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Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.

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 IC50 values ranging from 340 to 378 nM. Analogously, all the compounds were able to inhibit the self β-amyloid1-42 aggregation. The gallic acid hybrid GA2 as well as the 2-chromonecarboxylic acid hybrids CA1 and CA2 prevented the self-mediated Aβ 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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Nesi G,Chen Q,Sestito S,Digiacomo M,Yang X,Wang S,Pi R,Rapposelli S

doi

10.1016/j.ejmech.2017.10.006

subject

Has Abstract

pub_date

2017-12-01 00:00:00

pages

232-239

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30798-5

journal_volume

141

pub_type

杂志文章

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