مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

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Cites:

1

Information Journal Paper

Title

Coumarin derivatives bearing benzoheterocycle moiety: synthesis, cholinesterase inhibitory, and docking simulation study

Pages

  631-638

Abstract

 Objective(s): To investigate the efficiency of a novel series of coumarin derivatives bearing benzoheterocycle moiety as novel cholinesterase inhibitors. Materials and Methods: Different 7-hydroxycoumarin derivatives were synthesized via Pechmann or Knoevenagel condensation and conjugated to different benzoheterocycle (8-hydroxyquinoline, 2-mercaptobenzoxazole or 2-mercaptobenzimidazole) using dibromoalkanes 3a-m. Final compounds were evaluated against Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) by Ellman's method. Kinetic study of AChE inhibition and ligand-protein docking simulation were also carried out for the most potent compound 3b. Results: Some of the compounds revealed potent and selective activity against AChE. Compound 3b containing the quinoline group showed the best activity with an IC50 value of 8. 80 μ M against AChE. Kinetic study of AChE inhibition revealed the mixed-type inhibition of the enzyme by compound 3b. Ligand-protein docking simulation also showed that the flexibility of the hydrophobic five carbons linker allows the quinoline ring to form π-π interaction with Trp279 in the PAS. Conclusion: We suggest these synthesized compounds could become potential leads for AChE inhibition and prevention of AD symptoms.

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    • Cite

    APA: Copy

    Hirbod, Kimia, Jalili baleh, Leili, NADRI, HAMID, ebrahimi, Seyed esmaeil Sadat, MORADI, ALIREZA, PAKSERESHT, BAHAR, FOROUMADI, ALIREZA, SHAFIEE, ABBAS, & KHOOBI, MEHDI. (2017). Coumarin derivatives bearing benzoheterocycle moiety: synthesis, cholinesterase inhibitory, and docking simulation study. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 20(6), 631-638. SID. https://sid.ir/paper/726647/en

    Vancouver: Copy

    Hirbod Kimia, Jalili baleh Leili, NADRI HAMID, ebrahimi Seyed esmaeil Sadat, MORADI ALIREZA, PAKSERESHT BAHAR, FOROUMADI ALIREZA, SHAFIEE ABBAS, KHOOBI MEHDI. Coumarin derivatives bearing benzoheterocycle moiety: synthesis, cholinesterase inhibitory, and docking simulation study. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES[Internet]. 2017;20(6):631-638. Available from: https://sid.ir/paper/726647/en

    IEEE: Copy

    Kimia Hirbod, Leili Jalili baleh, HAMID NADRI, Seyed esmaeil Sadat ebrahimi, ALIREZA MORADI, BAHAR PAKSERESHT, ALIREZA FOROUMADI, ABBAS SHAFIEE, and MEHDI KHOOBI, “Coumarin derivatives bearing benzoheterocycle moiety: synthesis, cholinesterase inhibitory, and docking simulation study,” IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, vol. 20, no. 6, pp. 631–638, 2017, [Online]. Available: https://sid.ir/paper/726647/en

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