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Synthesis of some new 3-coumaranone and coumarin derivatives as dual inhibitors of acetyl- and butyrylcholinesterase.
Arch Pharm (Weinheim). 2013 Aug; 346(8):577-87.AP

Abstract

A novel series of coumarin and 3-coumaranone derivatives encompassing the phenacyl pyridinium moiety were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity using Ellman's method. All compounds presented inhibitory activity against both AChE and BuChE in the micromolar range. The molecular docking simulations revealed that all compounds were dual binding site inhibitors of AChE. A kinetic study was performed and the mechanism of enzyme inhibition was proved to be of mixed type. All compounds were tested for their antioxidant activity and no significant activity was observed.

Authors+Show Affiliations

School of Chemistry, University College of Science, University of Tehran, Tehran, Iran.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

23852709

Citation

Alipour, Masoumeh, et al. "Synthesis of some New 3-coumaranone and Coumarin Derivatives as Dual Inhibitors of Acetyl- and Butyrylcholinesterase." Archiv Der Pharmazie, vol. 346, no. 8, 2013, pp. 577-87.
Alipour M, Khoobi M, Nadri H, et al. Synthesis of some new 3-coumaranone and coumarin derivatives as dual inhibitors of acetyl- and butyrylcholinesterase. Arch Pharm (Weinheim). 2013;346(8):577-87.
Alipour, M., Khoobi, M., Nadri, H., Sakhteman, A., Moradi, A., Ghandi, M., Foroumadi, A., & Shafiee, A. (2013). Synthesis of some new 3-coumaranone and coumarin derivatives as dual inhibitors of acetyl- and butyrylcholinesterase. Archiv Der Pharmazie, 346(8), 577-87. https://doi.org/10.1002/ardp.201300080
Alipour M, et al. Synthesis of some New 3-coumaranone and Coumarin Derivatives as Dual Inhibitors of Acetyl- and Butyrylcholinesterase. Arch Pharm (Weinheim). 2013;346(8):577-87. PubMed PMID: 23852709.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis of some new 3-coumaranone and coumarin derivatives as dual inhibitors of acetyl- and butyrylcholinesterase. AU - Alipour,Masoumeh, AU - Khoobi,Mehdi, AU - Nadri,Hamid, AU - Sakhteman,Amirhossein, AU - Moradi,Alireza, AU - Ghandi,Mehdi, AU - Foroumadi,Alireza, AU - Shafiee,Abbas, Y1 - 2013/07/15/ PY - 2013/03/08/received PY - 2013/04/10/revised PY - 2013/04/12/accepted PY - 2013/7/16/entrez PY - 2013/7/16/pubmed PY - 2014/1/23/medline KW - 3-Coumaranone KW - Actylcholinesterase KW - Butyrylcholinesterase KW - Coumarin KW - Docking study KW - Phenacyl pyridinium SP - 577 EP - 87 JF - Archiv der Pharmazie JO - Arch Pharm (Weinheim) VL - 346 IS - 8 N2 - A novel series of coumarin and 3-coumaranone derivatives encompassing the phenacyl pyridinium moiety were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity using Ellman's method. All compounds presented inhibitory activity against both AChE and BuChE in the micromolar range. The molecular docking simulations revealed that all compounds were dual binding site inhibitors of AChE. A kinetic study was performed and the mechanism of enzyme inhibition was proved to be of mixed type. All compounds were tested for their antioxidant activity and no significant activity was observed. SN - 1521-4184 UR - https://www.unboundmedicine.com/medline/citation/23852709/Synthesis_of_some_new_3_coumaranone_and_coumarin_derivatives_as_dual_inhibitors_of_acetyl__and_butyrylcholinesterase_ L2 - https://doi.org/10.1002/ardp.201300080 DB - PRIME DP - Unbound Medicine ER -