Synthesis and Anticholinesterase Evaluation of Cassine, Spectaline and Analogues
In this work, twelve analogues of piperidine alkaloids (-)-cassine and (-)-spectaline were synthesized, as well as the racemic forms of these natural products. The compounds were evaluated for their inhibition of electric eel acetylcholinesterase (AChE<sub>ee</sub>) and human butyrylchol...
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| Main Authors: | , , , |
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| Format: | Book |
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MDPI AG,
2022-10-01T00:00:00Z.
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| Summary: | In this work, twelve analogues of piperidine alkaloids (-)-cassine and (-)-spectaline were synthesized, as well as the racemic forms of these natural products. The compounds were evaluated for their inhibition of electric eel acetylcholinesterase (AChE<sub>ee</sub>) and human butyrylcholinesterase (BChE<sub>hu</sub>) by on-flow mass-spectrometry-based dual-enzyme assay, and the inhibition mechanisms for the most potent analogues were also determined. Our results showed a preference for BChE<sub>hu</sub> inhibition with compounds <b>10c</b> (Ki = 5.24 μM), <b>12b</b> (Ki = 17.4 μM), <b>13a</b> (Ki = 13.2 μM) and <b>3</b> (Ki = 11.3 μM) displaying the best inhibitory activities. |
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| Item Description: | 10.3390/scipharm90040063 2218-0532 0036-8709 |