AI Article Synopsis
- Pyrazole-fused phenanthroline compounds were synthesized and characterized using various techniques like NMR and X-ray diffraction.
- Compounds were tested as inhibitors for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with compound 5c showing the best activity against AChE and compound 5l against BChE.
- Additionally, several compounds demonstrated effective cationic radical scavenging abilities, particularly compounds 5e, 5f, and 5g, while 71% of the compounds exhibited good oral bioavailability based on Lipinski's rules.
Article Abstract
Pyrazole-fused phenanthroline compounds were obtained through several synthetic routes. NMR, HRMS, and IR techniques were used to characterize and confirm the chemical structures. Crystal structures were obtained from compounds 3a, 5b, 5j, 5k, and 5n and analyzed using X-ray diffraction. Compounds were evaluated as acetyl (AChE) and butyrylcholinesterase (BChE) inhibitors, and the results showed a moderate activity. Compound 5c presented the best activity against AChE (IC = 53.29 μM) and compound 5l against BChE enzyme (IC = 119.3 μM). Furthermore, the ability of the synthetic compounds to scavenge cationic radicals DPPH and ABTS was evaluated. Compound 5e (EC = 26.71 μg mL) presented the best results in the DPPH assay, and compounds 5e, 5f and 5g (EC = 11.51, 3.10 and <3 μg mL, respectively) showed better ABTS cationic radical scavenging results. Finally, analyses indicated that 71% of the compounds show good oral availability and are within the ranges established by the Lipinski criteria.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9671100 | PMC |
| http://dx.doi.org/10.1039/d2ra05532e | DOI Listing |
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