AI Article Synopsis
- The study developed a series of 8-hydroxy-2,7-naphthyridin-2-ium salts based on the natural compound chelerythrine, which inhibits key enzymes AChE and BChE.
- Spectroscopic analyses confirmed the zwitterionic properties of the new compounds and helped identify their neutral state.
- Some compounds emerged as dual inhibitors of AChE and BChE, while others preferred AChE, with structural characteristics linked to their biological activity identified through further studies.
Article Abstract
By analogy with the natural product chelerythrine, which has been identified as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), we prepared a small series of 8-hydroxy-2,7-naphthyridin-2-ium salts. Spectroscopic analyses allowed us to elucidate the zwitterionic nature of 2,7-naphthyridin-1(7)-ones, the neutral state of 8-hydroxy-2,7-naphthyridin-2-ium salts. Among the tested compounds, we identified dual inhibitors of AChE and BChE as well as an inhibitor showing a preferential inhibition of AChE over BChE. By characterization in combination with docking studies, we were able to identify structural features that influence the biological activity of 8-hydroxy-2,7-naphthyridin-2-ium salts.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072306 | PMC |
| http://dx.doi.org/10.1039/c6md00647g | DOI Listing |
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