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SAR based in-vitro anticholinesterase and molecular docking studies of nitrogenous progesterone derivatives

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SAR based in-vitro anticholinesterase and molecular docking studies of nitrogenous progesterone derivatives. / Amin, Muafia Jabeen; Miana, Ghulam Abbas; Rashid, Umer; Rahman, Khondaker Miraz; Khan, Hidayat-ullah; Sadiq, Abdul.

In: Steroids, Vol. 158, 108599, 06.2020, p. 1-11.

Research output: Contribution to journalArticle

Harvard

Amin, MJ, Miana, GA, Rashid, U, Rahman, KM, Khan, H & Sadiq, A 2020, 'SAR based in-vitro anticholinesterase and molecular docking studies of nitrogenous progesterone derivatives', Steroids, vol. 158, 108599, pp. 1-11. https://doi.org/10.1016/j.steroids.2020.108599

APA

Amin, M. J., Miana, G. A., Rashid, U., Rahman, K. M., Khan, H., & Sadiq, A. (2020). SAR based in-vitro anticholinesterase and molecular docking studies of nitrogenous progesterone derivatives. Steroids, 158, 1-11. [108599]. https://doi.org/10.1016/j.steroids.2020.108599

Vancouver

Amin MJ, Miana GA, Rashid U, Rahman KM, Khan H, Sadiq A. SAR based in-vitro anticholinesterase and molecular docking studies of nitrogenous progesterone derivatives. Steroids. 2020 Jun;158:1-11. 108599. https://doi.org/10.1016/j.steroids.2020.108599

Author

Amin, Muafia Jabeen ; Miana, Ghulam Abbas ; Rashid, Umer ; Rahman, Khondaker Miraz ; Khan, Hidayat-ullah ; Sadiq, Abdul. / SAR based in-vitro anticholinesterase and molecular docking studies of nitrogenous progesterone derivatives. In: Steroids. 2020 ; Vol. 158. pp. 1-11.

Bibtex Download

@article{f51ec63d72e143dea2a653876bf7b8b9,
title = "SAR based in-vitro anticholinesterase and molecular docking studies of nitrogenous progesterone derivatives",
abstract = "Progesterone is a steroidal hormone that has been described with pathogenic features of brain dysfunction, realized with advanced age-related neurodegenerative diseases such as Alzheimer{\textquoteright}s disease. In this study, sixteen nitrogenous derivatives of progesterone which we previously synthesized have been used for Alzheimer targets. The progesterone derivatives (1–16) were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potentials in a dose-dependent manner. All the compounds exhibited overwhelming AChE inhibitions, with IC50 values ranging from 14.40 to 40.37 μM. Similarly, the BChE inhibitory potentials of our compounds were also dominant with IC50 values between 20.08 and 46.84 μM. In comparison to our compounds, the standard drug galantamine attain IC50 values of 12.03 and 18.20 μM against AChE and BChE respectively. Molecular docking studies suggested that the compounds exerted their inhibitory activity by binding to the active site of the enzyme. The cholinergic system plays an important role in the regulation of learning and memory processes and has been a major target for the design of anti-Alzheimer{\textquoteright}s drugs. Therefore, these nitrogen-containing progesterone derivatives will be of potential interest to researchers working in AD for developing new drugs or chemical tools to study the disease.",
author = "Amin, {Muafia Jabeen} and Miana, {Ghulam Abbas} and Umer Rashid and Rahman, {Khondaker Miraz} and Hidayat-ullah Khan and Abdul Sadiq",
year = "2020",
month = jun,
doi = "10.1016/j.steroids.2020.108599",
language = "English",
volume = "158",
pages = "1--11",
journal = "Steroids",
issn = "0039-128X",
publisher = "Elsevier Inc.",

}

RIS (suitable for import to EndNote) Download

TY - JOUR

T1 - SAR based in-vitro anticholinesterase and molecular docking studies of nitrogenous progesterone derivatives

AU - Amin, Muafia Jabeen

AU - Miana, Ghulam Abbas

AU - Rashid, Umer

AU - Rahman, Khondaker Miraz

AU - Khan, Hidayat-ullah

AU - Sadiq, Abdul

PY - 2020/6

Y1 - 2020/6

N2 - Progesterone is a steroidal hormone that has been described with pathogenic features of brain dysfunction, realized with advanced age-related neurodegenerative diseases such as Alzheimer’s disease. In this study, sixteen nitrogenous derivatives of progesterone which we previously synthesized have been used for Alzheimer targets. The progesterone derivatives (1–16) were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potentials in a dose-dependent manner. All the compounds exhibited overwhelming AChE inhibitions, with IC50 values ranging from 14.40 to 40.37 μM. Similarly, the BChE inhibitory potentials of our compounds were also dominant with IC50 values between 20.08 and 46.84 μM. In comparison to our compounds, the standard drug galantamine attain IC50 values of 12.03 and 18.20 μM against AChE and BChE respectively. Molecular docking studies suggested that the compounds exerted their inhibitory activity by binding to the active site of the enzyme. The cholinergic system plays an important role in the regulation of learning and memory processes and has been a major target for the design of anti-Alzheimer’s drugs. Therefore, these nitrogen-containing progesterone derivatives will be of potential interest to researchers working in AD for developing new drugs or chemical tools to study the disease.

AB - Progesterone is a steroidal hormone that has been described with pathogenic features of brain dysfunction, realized with advanced age-related neurodegenerative diseases such as Alzheimer’s disease. In this study, sixteen nitrogenous derivatives of progesterone which we previously synthesized have been used for Alzheimer targets. The progesterone derivatives (1–16) were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potentials in a dose-dependent manner. All the compounds exhibited overwhelming AChE inhibitions, with IC50 values ranging from 14.40 to 40.37 μM. Similarly, the BChE inhibitory potentials of our compounds were also dominant with IC50 values between 20.08 and 46.84 μM. In comparison to our compounds, the standard drug galantamine attain IC50 values of 12.03 and 18.20 μM against AChE and BChE respectively. Molecular docking studies suggested that the compounds exerted their inhibitory activity by binding to the active site of the enzyme. The cholinergic system plays an important role in the regulation of learning and memory processes and has been a major target for the design of anti-Alzheimer’s drugs. Therefore, these nitrogen-containing progesterone derivatives will be of potential interest to researchers working in AD for developing new drugs or chemical tools to study the disease.

U2 - 10.1016/j.steroids.2020.108599

DO - 10.1016/j.steroids.2020.108599

M3 - Article

VL - 158

SP - 1

EP - 11

JO - Steroids

JF - Steroids

SN - 0039-128X

M1 - 108599

ER -

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