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Design, synthesis, molecular modeling, in vitro evaluation of novel piperidine-containing hydrazone derivatives as cholinesterase inhibitors

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Tam Metin / Full Text (2.960Mb)

Erişim

info:eu-repo/semantics/closedAccess

Tarih

2024

Yazar

Tok, Fatih
Baltaş, Nimet
Abas, Burçin İrem
Tatar Yılmaz, Gizem
Kaya, Süleyman
Koçyiğit-Kaymakçıoğlu, Bedia
Çevik, Özge

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Künye

Tok, F., Baltaş, N., Abas, B. İ., Tatar Yılmaz, G., Kaya, S., Koçyiğit-Kaymakçıoğlu, B., & Çevik, Ö. (2024). Design, synthesis, molecular modeling, in vitro evaluation of novel piperidine-containing hydrazone derivatives as cholinesterase inhibitors. Drug development research, 85(5), e22240. https://doi.org/10.1002/ddr.22240

Özet

In an effort to develop new and effective therapeutic agents for Alzheimer's disease, a series of hydrazone derivatives bearing piperidine rings have been designed and synthesized. The chemical structures of the compounds were characterized by various spectroscopic techniques. In vitro antioxidant and cholinesterase activities of the compounds were evaluated. Among the compounds, N12 exhibited the most antioxidant activity in all methods (CUPRAC, FRAP, DPPH, ABTS). In vitro acetylcholinesterase (AChE) activity results of the compounds showed good IC50 values between 14.124 ± 0.084 and 49.680 ± 0.110 µM were obtained (IC50 = 38.842 ± 0.053 µM for Donepezil). Among the compounds, N7 and N6 are much more effective derivatives than the standard compound donepezil with IC50 values of 14.124 ± 0.084 and 17.968 ± 0.072 µM, respectively. In vitro, butyrylcholinesterase (BChE) inhibition values of the compounds were between 13.505 ± 0.025 and 52.230 ± 0.027 μm. Among the compounds, N6 has the highest BChE inhibition with an IC50 value of 13.505 μm in the series. The cytotoxicity and AChE inhibitory activity of the compounds on SH-SY5Y cell lines were also evaluated. Kinetic studies were also performed to determine the behavior of the compounds as competitive or noncompetitive inhibitors. The binding modes of N6, which was determined to be highly effective according to in vitro analyses, with AChE and BChE were investigated using molecular docking studies, and the stability of the complexes was determined by molecular dynamics simulations. These findings indicated that AChE and BChE enzymes maintained their overall structural stability and compactness during interactions with compound N6.

Kaynak

Design, synthesis, molecular modeling, in vitro evaluation of novel piperidine-containing hydrazone derivatives as cholinesterase inhibitors

Cilt

85

Sayı

5

Bağlantı

https://doi.org/10.1002/ddr.22240
https://hdl.handle.net/11436/9265

Koleksiyonlar

  • FEF, Kimya Bölümü Koleksiyonu [474]
  • PubMed İndeksli Yayınlar Koleksiyonu [2443]
  • Scopus İndeksli Yayınlar Koleksiyonu [5931]
  • WoS İndeksli Yayınlar Koleksiyonu [5260]



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