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Turkish Journal of Chemistry

2020

Acetylcholinesterase

Articles 1 - 3 of 3

Full-Text Articles in Physical Sciences and Mathematics

Synthesis And Bioactivities Of 1-(4-Hydroxyphenyl)-2-((Heteroaryl)Thio)Ethanones As Carbonic Anhydrase I, Ii And Acetylcholinesterase Inhibitors, Cem Yamali, Hali̇se İnci̇ Gül, Yeli̇z Demi̇r, Cavi̇t Kazaz, İlhami̇ Gülçi̇n Jan 2020

Synthesis And Bioactivities Of 1-(4-Hydroxyphenyl)-2-((Heteroaryl)Thio)Ethanones As Carbonic Anhydrase I, Ii And Acetylcholinesterase Inhibitors, Cem Yamali, Hali̇se İnci̇ Gül, Yeli̇z Demi̇r, Cavi̇t Kazaz, İlhami̇ Gülçi̇n

Turkish Journal of Chemistry

The discovery of enzyme targeting inhibitors is a popular area of drug research. Biological activities of the compounds bearing phenol and heteroaryl groups make them popular groups in drug design targeting important enzymes such as acetylcholinesterase (AChE, E.C.3.1.1.7) and carbonic anhydrases (CAs, EC 4.2.1.1). 1-(4-hydroxyphenyl)-2-((aryl)thio)ethanones as possible AChE and CAs inhibitors were synthesized, and their chemical structures were confirmed by IR, $^{1}$H NMR, $^{13}$C NMR, and HRMS. The compounds 2 and 4 were found potent AChE inhibitors with the Ki values of 22.13 ± 1.96 nM and 23.71 ± 2.95 nM, respectively, while the compounds 2 (Ki $=$ 8.61 ± …


New Sandwich-Type Polymeric Potassium-Dicyanoargentate(I) Complex: Synthesis, Characterization And Enzymatic Activity, Nesri̇n Korkmaz Jan 2020

New Sandwich-Type Polymeric Potassium-Dicyanoargentate(I) Complex: Synthesis, Characterization And Enzymatic Activity, Nesri̇n Korkmaz

Turkish Journal of Chemistry

Coordination compounds containing dicyanoargentate(I) have remarkable biological potential due to their therapeutic antibacterial, antifungal, antibiofilm, and anticancer properties. In this study, a new dicyanoargentate(I)-based complex was synthesized and characterized by various procedures (elemental, thermal, FT-IR for complex) involving crystal analysis of the complex. In addition, the biological activity of this new compound on the acetylcholinesterase (AChE) enzyme, an important enzyme for the nervous system, was investigated. When the infrared (IR) spectrum of the complex is examined, the OH vibration peak resulting from H$_{2}$O molecules in the structure at 3948-3337 cm$^{-1}$ and at 2138 cm$^{-1}$, along with a CN peak coordinated …


Synthesis And Pharmacological Effects Of Novel Benzenesulfonamides Carryingbenzamide Moiety As Carbonic Anhydrase And Acetylcholinesterase Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Bariş Anil, İlhami̇ Gülçi̇n Jan 2020

Synthesis And Pharmacological Effects Of Novel Benzenesulfonamides Carryingbenzamide Moiety As Carbonic Anhydrase And Acetylcholinesterase Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Bariş Anil, İlhami̇ Gülçi̇n

Turkish Journal of Chemistry

N-(1-(4-Methoxyphenyl)-3-oxo-3-((4-(N-(substituted)sulfamoyl)phenyl)amino)prop-1-en-1-yl)benzamides 3a - g were designed since sulfonamide and benzamide pharmacophores draw great attention in novel drug design due to their wide range of bioactivities including acetylcholinesterase (AChE) and human carbonic anhydrase I and II (hCA I and hCA II) inhibitory potencies. Structure elucidation of the compounds was carried out by 1H NMR, 13C NMR, and HRMS spectra. In vitro enzyme assays showed that the compounds had significant inhibitory potential against hCA I, hCA II, and AChE enzymes at nanomolar levels. Ki values were in the range of 4.07 ± 0.38 - 29.70 ± 3.18 nM for hCA I and …