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Design, synthesis and evaluation of new L-proline derivatives as acetylcholinesterase inhibitors

Tian, Y.-f.; Chen, J.-t.; Li, J.-j.; Zhang, Y.-c.; Cao, T.-t.; Ma, Z.-y.

Yao Xue Xue Bao 50(6): 719-724

2015

ISSN/ISBN: 0513-4870
PMID: 26521443
Document Number: 681384
In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.

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