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Abstract Title:

Piperlongumine B and analogs are promising and selective inhibitors for acetylcholinesterase.

Abstract Source:

Eur J Med Chem. 2017 Aug 2 ;139:222-231. Epub 2017 Aug 2. PMID: 28802122

Abstract Author(s):

Jana Wiemann, Julia Karasch, Anne Loesche, Lucie Heller, Wolfgang Brandt, René Csuk

Article Affiliation:

Jana Wiemann

Abstract:

Piperlongumine B (19), an alkaloid previously isolated from long pepper (Piper longum) has been synthesized for the first time in a short sequence and in good yield together with 19 analogs. Screening of these compounds in Ellman's assays showed several of them to be good inhibitors of acetylcholinesterase while being less active for butyrylcholinesterase. Activity of the compounds increased with the ring size of the heterocycle, and a maximum of activity was observed for an analog holding 12 methylene groups in the aliphatic side chain. These compounds may be regarded as promising candidates for the development of efficient inhibitors of acetylcholinesterase being useful for the treatment of Alzheimer's disease.

Study Type : In Vitro Study

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