Biological evaluation and molecular docking studies of 4-aminobenzohydrazide derivatives as cholinesterase inhibitors

Almaz, Zuleyha; Öztekіn, Aykut; Tan, Ayşe; Özdemir, Haşan

doi:10.1016/j.molstruc.2021.130918

Cited by 22 publications

(15 citation statements)

References 28 publications

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“…Almaz, Z. et al [ 36 ] investigated the inhibitory effects of several mono- or di-substituted 4-aminobenzohydrazide derivatives against AChE, exploiting the biological activities and the pharmacological effects of the benzohydrazide moiety. The most active derivatives were docked into the AChE active sites.…”

Section: Inhibitionmentioning

confidence: 99%

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A Review on Recent Approaches on Molecular Docking Studies of Novel Compounds Targeting Acetylcholinesterase in Alzheimer Disease

Peitzika

Pontiki

2023

Molecules

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Alzheimer’s disease (AD), a neurodegenerative brain disorder that affects millions of people worldwide, is characterized by memory loss and cognitive decline. Low levels of acetylcholine and abnormal levels of beta-amyloid, T protein aggregation, inflammation, and oxidative stress, have been associated with AD, and therefore, research has been oriented towards the cholinergic system and primarily on acetylcholinesterase (AChE) inhibitors. In this review, we are focusing on the discovery of AChE inhibitors using computer-based modeling and simulation techniques, covering the recent literature from 2018–2022. More specifically, the review discusses the structures of novel, potent acetylcholinesterase inhibitors and their binding mode to AChE, as well as the physicochemical requirements for the design of potential AChE inhibitors.

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Section: Inhibitionmentioning

confidence: 99%

“…The Phe293, His443, and Phe334 residues established -alkyl interactions with the Br substituent of its benzene ring. Furthermore, the compound’s benzene ring interacted in a π-T shape with the Trp82 and Tyr333 residues [ 36 ].…”

Section: Inhibitionmentioning

confidence: 99%

A Review on Recent Approaches on Molecular Docking Studies of Novel Compounds Targeting Acetylcholinesterase in Alzheimer Disease

Peitzika

Pontiki

2023

Molecules

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“…IC50 values were determined using GraphPad Prism 5 software by running an inhibitor curve against the normalization of the response (variable slope). IC50 is the concentration at which a substance exerts half of its maximum inhibitory effect (Almaz et al, 2021).…”

Section: Biochemical Studiesmentioning

confidence: 99%

Investigation of Cholinesterase Inhibitor Effects of Some Chalcone Substituted Metallophthalocyanines

Tekin

Arslan

2022

Karadeniz Fen Bilimleri Dergisi

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In this work, previously synthesized tetra-chalcone-substituted metallophthalocyanines (MPcs) containing Ni(II), Zn(II), Co(II), and Cu(II) in the inner core were investigated anticholinergic activities against Alzheimer's disease (AD). The MPcs were evaluated for their inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using the original Ellman's colorimetric procedure. Against these two cholinesterase enzymes, all compounds showed inhibitory effects with IC50 values ranging from 1.243-2.369 μM against AChE and 2.865-3.372 μM against BChE. Among the four MPcs, CuPcs (2) showed the strongest inhibitory activity against AChE. ZnPcs (3) also showed the most effective inhibition for BChE.

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“…Acetylcholinesterase (AChE) from Electric eel (Electrophorus electricus) and butyrylcholinesterase (BChE) from equine serum were obtained from Sigma-Aldrich (St. Louise, MO). The inhibitory effects of V. insulare extracts against AChE and BChE were measured using a slight modification of Ellman's spectrophotometric method [11] as described previously [12] and using commercially available galantamine as the reference compound. Acetylthiocholine iodide (AChI), butyrylthiocholine iodide (BChI) were used as the substrate in the reaction, 5′dithiobis-2 -nitrobenzoic acid (DTNB) was used as Ellman's reagent were purchased from Sigma -Aldrich.…”

Section: Cholinesterase Inhibition Assaymentioning

confidence: 99%

Investigation of Anticholinesterase and Anticancer Effects of Verbascum insulare Boiss. Et Heldr. Extracts Growing in Mus Region

Alan

Almaz

2022

Bitlis Eren Üniversitesi Fen Bilimleri Dergisi

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Since the existence of humanity, plants have been used in many treatment methods. Members of the genus Verbascum, also known as mullein, a member of the Scrophulariaceae family, have been evaluated for their traditional use against various ailments. In this study, the anticholinesterase and anticancer activities of Verbascum member Verbascum insulare Boiss. Et Heldr. collected from Muş region were investigated. V. insulare leaf ethanol (L-EtOH), leaf purified water (L-PW), root ethanol (R-EtOH), and root purified water (R-PW) extracts were obtained. The anticancer activity of the extracts against HT-29, MCF-7, and L-929 cell lines was examined using the 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) test and the anticholinesterase activity was determined. It was found that the ethanol extract showed higher anticancer activity against cancer cell lines than the pure water extract and had more effective anticholinergic influences. No study has been found in the literature on the anticancer and anticholinesterase activity of this plant. Therefore, the results obtained from this study will contribute significantly to the development of herbal medicine in the future.

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Biological evaluation and molecular docking studies of 4-aminobenzohydrazide derivatives as cholinesterase inhibitors

Cited by 22 publications

References 28 publications

A Review on Recent Approaches on Molecular Docking Studies of Novel Compounds Targeting Acetylcholinesterase in Alzheimer Disease

A Review on Recent Approaches on Molecular Docking Studies of Novel Compounds Targeting Acetylcholinesterase in Alzheimer Disease

Investigation of Cholinesterase Inhibitor Effects of Some Chalcone Substituted Metallophthalocyanines

Investigation of Anticholinesterase and Anticancer Effects of Verbascum insulare Boiss. Et Heldr. Extracts Growing in Mus Region

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