Journals / Hacettepe Journal of Biology and Chemistry / 2022 / Cilt: 50 - Sayı: 2

Synthesis, Characterization, Investigation of AChE Activities and Molecular Docking Studies of New Schiff Bases Based on Substitute Salicyl Aldehyde

Subtitüe Salisil Aldehit Temelli Yeni Schiff Bazlarının Sentezi, Karakterizasyonu, AChE Aktivitelerinin İncelenmesi ve Moleküler Yerleştirme Çalışmaları

Pages
185–192
Publication Date
2022-10-17
DOI
—
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

According to the results obtained, the activities of compounds 4 (IC50: 1.396 ± 0.35 M) and 5 (IC50: 0.795 ± 0.47M) were found to be significantly effective than Tacrin (TAC) (IC50: 166.10 ± 17.53 M) (currently used drug).

📌 3 Key Takeaways

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Objective & Hypothesis:In this study, two new Schiff base compounds (4 and 5) based on substituted salicyl aldehyde were synthesized.
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Key Findings & Data:The structures of the synthesized compounds were determined by FT-IR and 1H(13C) NMR spectroscopies.
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Conclusion & Impact:According to the results obtained, the activities of compounds 4 (IC50: 1.396 ± 0.35 M) and 5 (IC50: 0.795 ± 0.47M) were found to be significantly effective than Tacrin (TAC) (IC50: 166.10 ± 17.53 M) (currently used drug).
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Schiff bazı · AChE inhibisyon aktivitesi · moleküler yerleştirme

Abstract

In this study, two new Schiff base compounds (4 and 5) based on substituted salicyl aldehyde were synthesized. The structures of the synthesized compounds were determined by FT-IR and 1H(13C) NMR spectroscopies. The AChE inhibition activities of the compounds were investigated. According to the results obtained, the activities of compounds 4 (IC50: 1.396 ± 0.35 M) and 5 (IC50: 0.795 ± 0.47M) were found to be significantly effective than Tacrin (TAC) (IC50: 166.10 ± 17.53 M) (currently used drug). The interaction types and binding energies of compound 5, which has higher activity, were investigated by molecular docking studies.

Özet

Bu çalışmada, substitute salisil aldehit temelli yeni Schiff bazları (4 ve 5) sentezlendi. Sentezlenen bileşiklerin yapıları FT-IR, 1H(13C) NMR spektroskopileri ile aydınlatıldı. Bileşiklerin AChE inhibisyon aktiviteleri araştırıldı. Elde edilen sonuçlara göre 4 (IC50: 1.396 ± 0.35 M) ve 5 (IC50: 0.795 ± 0.47M) bileşiklerinin aktiviteleri standart olarak kullanılan Tacrinden (TAC) (IC50: 166.10 ± 17.53 M) çok daha yüksek inhibisyon aktivitesi sergilemiştir. Yüksek aktiviteye sahip olan bileşik 5’in moleküler docking çalışmaları ile etkileşim türleri ve bağlanma enerjileri hesaplanmıştır.

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Cite This Article

ŞAHİN, İ. (2022). Synthesis, Characterization, Investigation of AChE Activities and Molecular Docking Studies of New Schiff Bases Based on Substitute Salicyl Aldehyde. Hacettepe Journal of Biology and Chemistry, Cilt: 50 - Sayı: 2, 185–192. https://ajindex.com/articles/528907

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References (14)

  1. C.M. Da Silva et al., Schiff bases: A short review of their antimicrobial activities, J. Adv. Res. 2 (1) (2011) 1–8.
  2. F.N. Ejiah et al., Substituent effect on spectral and antimicrobial activity of Schiff bases derived from aminobenzoic acids, Adv. Biol. Chem. 03 (05) (2013) 475–479.
  3. H.R. Afzal et al., Schiff Bases of Pioglitazone Provide Better Antidiabetic and Potent Antioxidant Effect in a Streptozotocin-Nicotinamide-Induced Diabetic Rodent Model, ACS Omega 6 (6) (2021) 4470–4479.
  4. P. Przybylski et al., Biological Properties of Schiff Bases and Azo Derivatives of Phenols, Curr. Org. Chem. 13 (2) (2009) 124–148.
  5. F.S. Tokalı et al., Synthesis, characterization, biological activity and molecular docking studies of novel schiff bases derived from thiosemicarbazide: Biochemical and computational approach, J. Mol. Struct. 1231 (2021).
  6. S. Onur et al., Synthesis, characterization and antibacterial effect of diarylmethylamine-based imines, J. Mol. Struct. 1214 (2020).
  7. S. Onur et al., New imino-methoxy derivatives: design, synthesis, characterization, antimicrobial activity, DNA interaction and molecular docking studies, J. Biomol. Struct. Dyn. 0 (0) (2021) 1–13.
  8. G. Bringmann et al., Full Papers, 67 (5) (2004) 5–10.
  9. S. Afrin Dalia et al., A short review on chemistry of schiff base metal complexes and their catalytic application, ~ 2859 ~ Int. J. Chem. Stud. 6 (3) (2018) 2859–2866.
  10. C. Jang et al., Identification of novel acetylcholinesterase inhibitors designed by pharmacophore-based virtual screening, molecular docking and bioassay, Sci. Rep. 8 (1) (2018) 1–21.
  11. E. Beal, Alzheimer disease:, Nat. Rev. Neurol. 7 (9) (2011) 474. Alzheimer’s Association, 2021 Alzheimer’s disease facts and figures special report Race, Ethnicity and Alzheimer’s in America, Alzheimers. Dement. 17 (3) (2021) 327–406. A. Rønneberg et al., The Editor recommends this issue’s article to the reader, Int. J. Paediatr. Dent. 29 (6) (2019) 683. S. Duong, T. Patel, and F. Chang, Dementia: What pharmacists need to know, Can. Pharm. J. 150 (2) (2017) 118–129.
  12. R.G. Jahn, Introduction, Role Conscious. Phys. World (2019) 1–5.
  13. H.R. Brunnström and E.M. Englund, Cause of death in patients with dementia disorders, Eur. J. Neurol. 16 (4) (2009) 488–492. J. Massoulié et al., Molecular and cellular biology of cholinesterases, Prog. Neurobiol. 41 (1) (1993) 31–91.
  14. M.S. More et al., Metal complexes driven from Schiff bases and semicarbazones for biomedical and allied applications: a review, Mater. Today Chem. 14