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Synthesis and cholinesterase inhibitory activity study of new piperidone grafted spiropyrrolidines.
Bioorg Chem. 2017 12; 75:210-216.BC

Abstract

Alzheimer's disease (AD) is a prevalent neurodegenerative disorder, which affected 35 million people in the world. The most practiced approach to improve the life expectancy of AD patients is to increase acetylcholine neurotransmitter level at cholinergic synapses by inhibition of cholinesterase enzymes. A series of unreported piperidone grafted spiropyrrolidines 8(a-p) were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Therein, compounds 8h and 8l displayed more potent AChE enzyme inhibition than standard drug with IC50 values of 1.88 and 1.37 µM, respectively. Molecular docking simulations for 8l possessing the most potent AChE inhibitory activities, disclosed its interesting binding templates to the active site channel of AChE enzymes. These compounds are remarkable AChE inhibitors and have potential as AD drugs.

Authors+Show Affiliations

School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia; Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE 68198, United States.College of Pharmacy, Al-Mustansiriyah University, 10001 Baghdad, Iraq.College of Education for Women, University of Anbar, 31001 Ramadi, Anbar, Iraq.School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia.Department of Chemistry, College of Sciences, King Saud University, PO Box 2455, Riyadh, Saudi Arabia. Electronic address: sraju@ksu.edu.sa.Department of Chemistry, College of Sciences, King Saud University, PO Box 2455, Riyadh, Saudi Arabia.Department of Chemistry, College of Sciences, King Saud University, PO Box 2455, Riyadh, Saudi Arabia.School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia. Electronic address: dr.Murugaiyah@gmail.com.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

28987876

Citation

Basiri, Alireza, et al. "Synthesis and Cholinesterase Inhibitory Activity Study of New Piperidone Grafted Spiropyrrolidines." Bioorganic Chemistry, vol. 75, 2017, pp. 210-216.
Basiri A, Abd Razik BM, Ezzat MO, et al. Synthesis and cholinesterase inhibitory activity study of new piperidone grafted spiropyrrolidines. Bioorg Chem. 2017;75:210-216.
Basiri, A., Abd Razik, B. M., Ezzat, M. O., Kia, Y., Kumar, R. S., Almansour, A. I., Arumugam, N., & Murugaiyah, V. (2017). Synthesis and cholinesterase inhibitory activity study of new piperidone grafted spiropyrrolidines. Bioorganic Chemistry, 75, 210-216. https://doi.org/10.1016/j.bioorg.2017.09.019
Basiri A, et al. Synthesis and Cholinesterase Inhibitory Activity Study of New Piperidone Grafted Spiropyrrolidines. Bioorg Chem. 2017;75:210-216. PubMed PMID: 28987876.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and cholinesterase inhibitory activity study of new piperidone grafted spiropyrrolidines. AU - Basiri,Alireza, AU - Abd Razik,Basma M, AU - Ezzat,Mohammed Oday, AU - Kia,Yalda, AU - Kumar,Raju Suresh, AU - Almansour,Abdulrahman I, AU - Arumugam,Natarajan, AU - Murugaiyah,Vikneswaran, Y1 - 2017/09/29/ PY - 2017/07/21/received PY - 2017/09/25/revised PY - 2017/09/28/accepted PY - 2017/10/11/pubmed PY - 2017/12/14/medline PY - 2017/10/9/entrez KW - AChE and BChE activities KW - Ionic liquid KW - Molecular docking KW - Spiropyrrolidines SP - 210 EP - 216 JF - Bioorganic chemistry JO - Bioorg. Chem. VL - 75 N2 - Alzheimer's disease (AD) is a prevalent neurodegenerative disorder, which affected 35 million people in the world. The most practiced approach to improve the life expectancy of AD patients is to increase acetylcholine neurotransmitter level at cholinergic synapses by inhibition of cholinesterase enzymes. A series of unreported piperidone grafted spiropyrrolidines 8(a-p) were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Therein, compounds 8h and 8l displayed more potent AChE enzyme inhibition than standard drug with IC50 values of 1.88 and 1.37 µM, respectively. Molecular docking simulations for 8l possessing the most potent AChE inhibitory activities, disclosed its interesting binding templates to the active site channel of AChE enzymes. These compounds are remarkable AChE inhibitors and have potential as AD drugs. SN - 1090-2120 UR - https://www.unboundmedicine.com/medline/citation/28987876/Synthesis_and_cholinesterase_inhibitory_activity_study_of_new_piperidone_grafted_spiropyrrolidines_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0045-2068(17)30545-X DB - PRIME DP - Unbound Medicine ER -