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Full-Text Articles in Physical Sciences and Mathematics
Evaluation Of Carbonic Anhydrase And Paraoxonase Inhibition Activities And Molecular Docking Studies Of Highly Water-Soluble Sulfonated Phthalocyanines, Emre Güzel, Fati̇h Sönmez, Sultan Erkan, Kübra Çikrikci, Adem Ergün, Nahi̇t Gençer, Oktay Arslan, Makbule Koçak
Evaluation Of Carbonic Anhydrase And Paraoxonase Inhibition Activities And Molecular Docking Studies Of Highly Water-Soluble Sulfonated Phthalocyanines, Emre Güzel, Fati̇h Sönmez, Sultan Erkan, Kübra Çikrikci, Adem Ergün, Nahi̇t Gençer, Oktay Arslan, Makbule Koçak
Turkish Journal of Chemistry
The investigation of carbonic anhydrase and paraoxonase enzyme inhibition properties of water-soluble zinc and gallium phthalocyanine complexes (1 and 2) are reported for the first time. The binding of p-sulfonylphenoxy moieties to the phthalocyanine structure favors excellent solubilities in water, as well as providing an inhibition effect on carbonic anhydrase (CA) I and II isoenzymes and paraoxonase (PON1) enzyme. According to biological activity results, both complexes inhibited hCA I, hCA II, and PON1. Whereas 1 and 2 showed moderate hCA I and hCA II (off-target cytosolic isoforms) inhibitory activity (Ki values of 26.09 μM and 43.11 μM for hCA I …
Synthesis And Pharmacological Effects Of Novel Benzenesulfonamides Carryingbenzamide Moiety As Carbonic Anhydrase And Acetylcholinesterase Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Bariş Anil, İlhami̇ Gülçi̇n
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 …