A novel series of 1,2,3-triazole-genipin analogues were designed, synthesized, and evaluated for neuroprotective activity, acetylcholinesterase (AChE), and butyrylcholinesterase (BuChE) inhibitory activity. The genipin analogues bearing bromoethyl- and diphenylhydroxy-triazole showed neuroprotective properties against HO toxicity along with potent inhibitory activity on BuChE with IC values of 31.77 and 54.33 μM, respectively, compared with galantamine (IC = 34.05 μM). The molecular docking studies of these genipin analogues showed good binding energy and interact well with the key amino acids of BuChE hydrogen-bonding and hydrophobic interactions. Triazole genipins might be promising lead compounds as anti-Alzheimer's agents.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9301951 | PMC |
| http://dx.doi.org/10.1021/acsomega.2c01593 | DOI Listing |
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