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

video

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

sound

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

Persian Version

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

View:

218
مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Download:

133
مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Cites:

Information Journal Paper

Title

2-(2-(4-Benzoylpiperazin-1-yl)ethyl)isoindoline-1, 3-dione derivatives: Synthesis, docking and acetylcholinesterase inhibitory evaluation as anti-alzheimer agents

Pages

  59-66

Abstract

 Alzheimer’ s disease (AD) as progressive cognitive decline and the most common form of dementia is due to degeneration of the cholinergic neurons in the brain. Therefore, administration of the Acetylcholinesterase (AChE) inhibitors such as donepezil is the first choice for treatment of the AD. In the present study, we focused on the Synthesis and anti-cholinesterase evaluation of new donepezil like analogs. Materials and Methods: A new series of Phthalimide derivatives (compounds 4a-4j) were synthesized via Gabriel protocol and subsequently amidation reaction was performed using various benzoic acid derivatives. Then, the corresponding anti-Acetylcholinesterase activity of the prepared derivatives (4a-4j) was assessed by utilization of the Ellman's test and obtained results were compared to donepezil. Besides, Docking study was also carried out to explore the likely in silico binding interactions. Results: According to the obtained results, electron withdrawing groups (Cl, F) at position 3 and an electron donating group (methoxy) at position 4 of the phenyl ring enhanced the Acetylcholinesterase inhibitory activity. Compound 4e (m-Fluoro, IC50 = 7. 1 nM) and 4i (p-Methoxy, IC50 = 20. 3 nM) were the most active compounds in this series and exerted superior potency than donepezil (410 nM). Moreover, a similar binding mode was observed in silico for all ligands in superimposition state with donepezil into the active site of Acetylcholinesterase. Conclusion: Studied compounds could be potential leads for discovery of novel anti-Alzheimer agents in the future.

Cites

  • No record.

    • References

  • No record.

    • Cite

    APA: Copy

    Abdi, NASIBEH, MORADI, ALIREZA, & ALIABADI, ALIREZA. (2017). 2-(2-(4-Benzoylpiperazin-1-yl)ethyl)isoindoline-1, 3-dione derivatives: Synthesis, docking and acetylcholinesterase inhibitory evaluation as anti-alzheimer agents. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 20(1), 59-66. SID. https://sid.ir/paper/720694/en

    Vancouver: Copy

    Abdi NASIBEH, MORADI ALIREZA, ALIABADI ALIREZA. 2-(2-(4-Benzoylpiperazin-1-yl)ethyl)isoindoline-1, 3-dione derivatives: Synthesis, docking and acetylcholinesterase inhibitory evaluation as anti-alzheimer agents. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES[Internet]. 2017;20(1):59-66. Available from: https://sid.ir/paper/720694/en

    IEEE: Copy

    NASIBEH Abdi, ALIREZA MORADI, and ALIREZA ALIABADI, “2-(2-(4-Benzoylpiperazin-1-yl)ethyl)isoindoline-1, 3-dione derivatives: Synthesis, docking and acetylcholinesterase inhibitory evaluation as anti-alzheimer agents,” IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, vol. 20, no. 1, pp. 59–66, 2017, [Online]. Available: https://sid.ir/paper/720694/en

    Related Journal Papers

  • No record.

    • Related Seminar Papers

  • No record.

    • Related Plans

  • No record.

    • Recommended Workshops






    Move to top
    telegram sharing button
    whatsapp sharing button
    linkedin sharing button
    twitter sharing button
    email sharing button
    email sharing button
    email sharing button
    sharethis sharing button