| Title : Synthesis, biological evaluation, and computational studies of N-benzyl pyridinium-curcumin derivatives as potent AChE inhibitors with antioxidant activity - Al-Rifai_2023_J.Enzyme.Inhib.Med.Chem_38_2281264 |
| Author(s) : Al-Rifai NM , Al-Khalileh NM , Zahra JA , El-Barghouthi MI , Darras FH |
| Ref : J Enzyme Inhib Med Chem , 38 :2281264 , 2023 |
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Abstract :
A library of N-benzylpyridinium-based compounds, 7a-j and 8a-j, was designed and synthesised as potential acetylcholinesterase) AChE (inhibitors. An in vitro assay for the synthesised compounds showed that most compounds had significant AChE inhibitory activities at the nanomolar and submicromolar levels. The benzyl (8a) and fluoro (8b) derivatives were the most active, with IC(50) values >=56 nM. Compound 7f, which had a benzyl moiety, showed the highest potency among all the target compounds, with an IC(50) value of 7.5 +/- 0.19 nM against AChE, which was higher than that of the activities of tacrine (IC(50) = 30 +/- 0.2 nM) and donepezil (IC(50) = 14 +/- 0.12 nM). Compounds with vanillin moieties exhibited antioxidant activity. Among the tested compounds, four derivatives (7f, 7 g, 8f, and 8 g) exhibited superior AChE inhibitory activity, with K(i) values of 6-16 nM, which were potent in the same range as the approved drug, donepezil. These compounds showed moderate antioxidant activities, as indicated by the results of the ABTS assay. |
| PubMedSearch : Al-Rifai_2023_J.Enzyme.Inhib.Med.Chem_38_2281264 |
| PubMedID: 37985494 |
Al-Rifai NM, Al-Khalileh NM, Zahra JA, El-Barghouthi MI, Darras FH (2023)
Synthesis, biological evaluation, and computational studies of N-benzyl pyridinium-curcumin derivatives as potent AChE inhibitors with antioxidant activity
J Enzyme Inhib Med Chem
38 :2281264
Al-Rifai NM, Al-Khalileh NM, Zahra JA, El-Barghouthi MI, Darras FH (2023)
J Enzyme Inhib Med Chem
38 :2281264