Acetylcholinesterase inhibition activity of some novel s-triazine derivatives

2016 ◽  
Vol 4 (Suppl. 3) ◽  
pp. A4.2
Author(s):  
Jovana Trifunović
Keyword(s):  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity ◽  
Triazine Derivatives

Synthesis and bioactivity of novel C2-glycosyl triazole derivatives as acetylcholinesterase inhibitors

2017 ◽  
Vol 23 (3) ◽  
pp. 231-236 ◽  
Author(s):  
Long Yin ◽  
Lei Wang ◽  
Xiu-Jian Liu ◽  
Feng-Chang Cheng ◽  
Da-Hua Shi ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Sodium Hydroxide ◽  
Acetylcholinesterase Inhibitors ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity ◽  
Triazole Derivatives ◽  
Inhibitory Activities ◽  
Ellman’S Method

AbstractNew C2-glycosyl triazole derivatives 6a–l were synthesized by cyclization of glycosyl acylthiosemicarbazides 5 in refluxing 3 N sodium hydroxide aqueous solution. Substrates 5 were obtained by the reaction of glycosyl isothiocyanate 3 with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of compounds 6 were tested by Ellman’s method. Compounds that exhibited over 85% inhibition were subsequently evaluated for the IC50 values. Compound 6f possesses the best acetylcholinesterase-inhibition activity with IC50 of 1.46±0.25 μg/mL.

Antioxidant, antiproliferative, and acetylcholinesterase inhibition activity of amino alcohol derivatives from 1,4-naphthoquinone

2020 ◽  
Vol 29 (11) ◽  
pp. 1986-1999
Author(s):  
Arturo Estolano-Cobián ◽  
Eduardo Noriega-Iribe ◽  
Laura Díaz-Rubio ◽  
José M. Padrón ◽  
Mirna Brito-Perea ◽  
...  
Keyword(s):  
Amino Alcohol ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity

scholarly journals New 1,3,5-Triazine Derivatives Incorporating Aminobenzenesulfonamide, Aminoalcohol, Piperazine, Chalcone or Stilbene Structural Motifs and Evaluation of Their Antioxidative Activity

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 17
Author(s):  
Eva Havránková ◽  
Nikola Čalkovská ◽  
Tereza Padrtová ◽  
Jozef Csöllei ◽  
Radka Opatřilová ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Ascorbic Acid ◽  
Antioxidative Activity ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Scavenging Activity ◽  
Inhibition Activity ◽  
Structural Motifs ◽  
Triazine Derivatives ◽  
Acidic Resin

A series of 1,3,5-triazine derivatives, incorporating aminobenzenesulfonamide, aminoalcohol/phenol, piperazine, chalcone, or stilbene structural motifs, were evaluated as potential antioxidants. The compounds were prepared by using step by step nucleophilic substitution of chlorine atoms in starting 2,4,6-trichloro-1,3,5-triazine. Reactions were catalyzed by Cu(I)-supported on a weakly acidic resin. The radical scavenging activity was determined in terms of %inhibition activity and IC50, using the ABTS method. Trolox and ascorbic acid (ASA) were used as standards. In the lowest used concentration 1 × 10−4 M, the %inhibition activity at time 0 min was comparable with both standards at least for 10 compounds. After 60 min compounds 1, 2, 9 and 25 showed nearly twice %inhibition (73.44–87.09%) in comparison with standards (Trolox = 41.49%; ASA = 31.07%). Values of IC50 correlated with %inhibition activity. For compounds 1, 2, 9 and 25 values of IC50 in time 60 min (17.16–27.78 μM) were 5 times lower than IC50 of both standards (Trolox = 178.33 μM; ASA = 147.47 μM). Based on these results, the presented 1,3,5-triazine derivatives and their analogs have a high potential in the treatment of illnesses caused or related to oxidative stress.

scholarly journals Chemical Composition and Acetylcholinesterase Inhibition Activity of Volatile Oil from Leaves of Arbutus unedo L. from Croatia

2019 ◽  
Vol 31 (5) ◽  
pp. 1110-1112
Author(s):  
O. Politeo ◽  
I. Ercegovic
Keyword(s):  
Chemical Composition ◽  
Volatile Oil ◽  
Acetylcholinesterase Inhibition ◽  
Nonanoic Acid ◽  
Inhibition Activity ◽  
Ache Inhibition ◽  
Arbutus Unedo ◽  
Lower Quantity

The volatile oil from leaves of Arbutus unedo L. from Croatia was subjected to chemical composition and acetylcholinesterase inhibition activity. The tested volatile oil was dominated by nonterpene compounds, with (E)-2-decenal, nonanal, nonanoic acid and octanol as main compounds. Terpene compounds were identified in lower quantity, with linalool and α-terpineol as main ones. Results showed low to moderate acetylcholinesterase (AChE) inhibition potential of tested oil, for tested concentration of 1 mg/mL.

scholarly journals Synthesis and Spectral Characterisation of (E)-3-(3-(4 (Dimethylamino)Phenyl)Acrylo-yl)-4-Hydroxy-2H-Chromen-2-One and Their Antibacterial Activity and Acetylcholinesterase Inhibition

2021 ◽  
Vol 2021 ◽  
pp. 1-15
Author(s):  
Ichraf Slimani ◽  
Naceur Hamdi ◽  
Sadeq M. Al-Hazmy ◽  
Ibrahim A. Alhagri ◽  
El-Zeiny M. Ebeid ◽  
...  
Keyword(s):  
Antimicrobial Properties ◽  
Emission Spectra ◽  
Coumarin Derivative ◽  
Dielectric Constants ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity ◽  
Enhanced Fluorescence ◽  
Spectral Characterisation ◽  
Molecular Rigidity ◽  
Fluorescent Stain

A new coumarin derivative, (E)-3-(3-(4-(dimethylamino) phenyl) acrylo-yl)-4-hydroxy-2H-chromen-2-one (3), was synthesized by the condensation of 3-acetyl-4-hydroxycoumarin (1) with 4-N,N-dimethylaminobenzaldehyde (2) in the presence of piperidine in ethanol. The structure of the synthesized compound was characterized using spectroscopic data (IR and 1H NMR) and elemental analysis. The antimicrobial properties and acetylcholinesterase inhibition activity (AChEI) of coumarin 3 were investigated, with the highest observed AChEI activity providing 48.25% inhibition. The electronic absorption and emission spectra revealed that 3 exists as two, main keto-enol tautomers. The ratios of these tautomers in both protic and aprotic solvents with different polarities and dielectric constants were calculated. The fluorescence of coumarin 3 was enhanced upon increasing the medium viscosity, which was due to the resultant molecular rigidity. This criterion was further investigated using DNA, whereby 3 showed enhanced fluorescence upon its uptake in DNA grooves and was therefore tested as a novel DNA fluorescent stain.

Synthesis and bioactivity of novel C2-glycosyl benzofuranylthiazoles derivatives as acetylcholinesterase inhibitors

2019 ◽  
Vol 43 (7-8) ◽  
pp. 257-261
Author(s):  
Lei Wang ◽  
Yu-Ran Wu ◽  
Shu-Ting Ren ◽  
Long Yin ◽  
You-Xian Wang ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Acetylcholinesterase Inhibitors ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity ◽  
Active Compounds ◽  
Inhibitory Activities ◽  
Ellman’S Method

A new series of C2-glycosyl benzofuranylthiazole derivatives was synthesised by the further cyclization of glycosyl thiourea and 2-(bromoacetyl)-benzofuran via Hantzsch’s method. The corresponding 2-(bromoacetyl)-benzofuran derivatives were obtained by the reaction from various salicylaldehydes, and the glycosyl thiourea was prepared through a series of steps from D-Glucosamine. The acetylcholinesterase-inhibitory activities of the products were tested by Ellman’s method. The most active compounds were subsequently evaluated for the 50% inhibitory concentration values. N-(1,3,4,6-tetra-O-benzyl-2-deoxy-β-D-glucopyranosyl)-4-(5-methoxy-benzofuran-2-yl)-1,3-thiazole-2-amine possessed the best acetylcholinesterase-inhibition activity with a 50% inhibitory concentration of 2.03 ± 0.26 μM.

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