In vitro inhibitory effects of some acetophenone derivatives on some metabolic enzymes and molecular docking

Taslimi, Parham

doi:10.1002/ardp.202000210

Cited by 3 publications

(3 citation statements)

References 65 publications

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“…proposed a method for determining the α‐glycosidase inhibitory properties of synthesized derivatives ( 1 ‐ 5 , 8 , 10 , 11 , 14 , 16 ‐ 19 , 21 ‐ 29 , 34 and 35 ) and this method was based on earlier research. At 405 nM, the absorbance was determined spectrophotometrically [70,71] . The IC 50 was calculated from activity (%) versus of synthesized derivatives ( 1 ‐ 5 , 8 , 10 , 11 , 14 , 16 ‐ 19 , 21 ‐ 29 , 34 and 35 ) concentration plots.…”

Section: Methodsmentioning

confidence: 99%

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Synthesis and Biological Activity of Some Bromophenols and Their Derivatives Including Natural Products

Menzek

Bayrak

Taslimi

et al. 2023

Chemistry & Biodiversity

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In addition to the first synthesis of the natural bromophenol butyl 2‐(3,5‐dibromo‐4‐hydroxyphenyl)acetate (1), indene derivatives 34 and 35 were synthesized from 3‐phenylpropenal derivatives in BBr3 medium. Five known natural bromophenols and some derivatives were synthesized by known methods. Cholinesterase (ChEs) inhibitors reduce the breakdown of acetylcholine and are used in the treatment of Alzheimer's disease (AD) and dementia symptoms. The inhibition effects of all obtained compounds were examined towards acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α‐glycosidase enzymes. All synthesized compounds demonstrated the strong inhibition effects against both cholinergic enzymes. For determination of Ki values of novel bromophenols Lineweaver‐Burk graphs were obtained. Ki values were found in the ranging of 0.13–14.74 nM for AChE, 5.11–23.95 nM for BChE, and 63.96–206.78 nM for α‐glycosidase, respectively. All bromophenols and their derivatives exhibit effective inhibition profile when compared to positive controls.

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Section: Methodsmentioning

confidence: 99%

“…At 405 nM, the absorbance was determined spectrophotometrically. [70,71] The IC 50 was calculated from activity (%) versus of synthesized derivatives (1-5, 8, 10, 11, 14, 16-19, 21-29, 34 and 35) concentration plots. Lineweaver-Burk graphs were used for the determination of K i and other inhibition parameters.…”

Section: α-Glycosidase Inhibition Studiesmentioning

confidence: 99%

Synthesis and Biological Activity of Some Bromophenols and Their Derivatives Including Natural Products

Menzek

Bayrak

Taslimi

et al. 2023

Chemistry & Biodiversity

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“…[20,21] In addition, AChE inhibitor compounds modulate ACh hydrolysis and also play an important role in diagnosing the cholinergic tone. [22,23] Type-2 diabetes mellitus (T2DM) is one of the most popular metabolic diseases in the world and is defined by hyperglycemia. α-Glucosidase enzymes are in the nutritive system that hydrolyzes carbohydrate molecules into glucose molecules.…”

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confidence: 99%

Synthesis and docking calculations of tetrafluoronaphthalene derivatives and their inhibition profiles against some metabolic enzymes

Erdoğan

Taslimi

Tüzün

2021

Archiv der Pharmazie

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Syntheses of tetrahydroepoxy, O-allylic, O-prenylic, and O-propargylic tetrafluoronaphthalene derivatives, starting from 1-bromo-2,3,4,5,6-pentafluorobenzene, are reported here for the first time. The O-substituted tetrafluoronaphthalene derivatives were designed and also synthesized via a one-pot nucleophilic substitution reaction in excellent yields, whereas the tetrafluorotetrahydroepoxynaphthalene derivate was synthesized via a reduction reaction in excellent yield. The chemical structures of all the synthesized molecules were characterized by nuclear magnetic resonance, infrared spectroscopy, and high-resolution mass spectrometry techniques.In this study, a series of novel tetrafluoronaphthalene derivatives (2, 2a, 4-6) was tested toward several enzymes including α-glucosidase, acetylcholinesterase (AChE), and human carbonic anhydrase I and II (hCA I/II). The tetrafluoronaphthalene deri-

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In vitro acetylcholinesterase, tyrosinase inhibitory potentials of secondary metabolites from Euphorbia schimperiana and Euphorbia balsamifera

Aljubiri

Elsalam

El-Hady

et al. 2022

Zeitschrift Für Naturforschung C

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Acetylcholinesterase, tyrosinase, and α-glucosidase inhibition activities of Euphorbia schimperiana and Euphorbia balsamifera extracts, fractions, and available pure compounds were evaluated for the first time. Acetylcholinesterase assay revealed a significant inhibitory activity of E. balsamifera total extract and n-hexane fraction with 47.7% and 43.3%, respectively, compared to the reference drug, which was 75%. The n-butanol fraction demonstrated tyrosinase inhibitory activity for E. balsamifera and E. schimperiana with 36.7% and 29.7%, respectively, compared to 60% for the reference drug. Quercetin-3-O-α-glucuronide, quercetin-3-O-β-D-glucuronide-methyl ester, quercetin-3-O-α-L-rhamnoside, 3,3′-di-O-methyl ellagic acid, 3,3′-di-O-methyl-ellagic acid-4-β-D-xylopyranoside, and 4-O-ethyl gallic acid were identified from E. schimperiana while quercetin-3-O-glucopyranoside and isoorientin were determined from E. balsamifera. The AChE inhibitory effect of pure compounds exhibited promising activity, where 4-O-ethylgallic acid demonstrated 51.1%, while the highest tyrosinase inhibition was demonstrated by isoorientin with 50.6% compared to the reference drug (60%). Finally, a molecular docking study was performed for the most promising AChE and tyrosinase inhibitors. The extracts, fractions, and isolated compounds showed no α-glucosidase inhibitory activity.

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In vitro inhibitory effects of some acetophenone derivatives on some metabolic enzymes and molecular docking

Abstract: In this study, the acetophenone derivatives 1-6 were found to be effective inhibitor molecules for α-glycosidase, human carbonic anhydrases I and II (hCA I/II), and acetylcholinesterase (AChE), with K i values in the range of 167.98 ± 25.06 to

Cited by 3 publications

References 65 publications

Synthesis and Biological Activity of Some Bromophenols and Their Derivatives Including Natural Products

Synthesis and Biological Activity of Some Bromophenols and Their Derivatives Including Natural Products

Synthesis and docking calculations of tetrafluoronaphthalene derivatives and their inhibition profiles against some metabolic enzymes

In vitro acetylcholinesterase, tyrosinase inhibitory potentials of secondary metabolites from Euphorbia schimperiana and Euphorbia balsamifera

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