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Full-Text Articles in Chemistry
Novel Mannich Bases With Strong Carbonic Anhydrases And Acetylcholinesterase Inhibition Effects: 3-(Aminomethyl)-6-{3-[4-(Trifluoromethyl)Phenyl]Acryloyl}-2(3h)- Benzoxazolones, Si̇nan Bi̇lgi̇ner, Bariş Anil, Mehmet Koca, Yeli̇z Demi̇r, İlhami̇ Gülçi̇n
Novel Mannich Bases With Strong Carbonic Anhydrases And Acetylcholinesterase Inhibition Effects: 3-(Aminomethyl)-6-{3-[4-(Trifluoromethyl)Phenyl]Acryloyl}-2(3h)- Benzoxazolones, Si̇nan Bi̇lgi̇ner, Bariş Anil, Mehmet Koca, Yeli̇z Demi̇r, İlhami̇ Gülçi̇n
Turkish Journal of Chemistry
In this study, a new series of Mannich bases, 3-(aminomethyl)-6-{3-[4-(trifluoromethyl)phenyl]acryloyl}-2(3H)- benzoxazolones (1a-g), were synthesized by the Mannich reaction. Inhibitory effects of the newly synthesized compounds towards carbonic anhydrases (CAs) and acetylcholinesterase (AChE) enzymes were evaluated to find out new potential drug candidate compounds. According to the inhibitory activity results, Ki values of the compounds 1 and 1a-g were in the range of 12.3 ± 1.2 to 154.0 ± 9.3 nM against hCA I, and they were in the range of 8.6 ± 1.9 to 41.0 ± 5.5 nM against hCA II. Ki values of acetazolamide (AZA) that was used as …
Synthesis And Biological Evaluation Of New Pyrazolebenzene-Sulphonamides As Potentialanticancer Agents And Hca I And Ii Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Hi̇roshi̇ Sakagami̇, Rüya Kaya, İlhami̇ Gülçi̇n
Synthesis And Biological Evaluation Of New Pyrazolebenzene-Sulphonamides As Potentialanticancer Agents And Hca I And Ii Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Hi̇roshi̇ Sakagami̇, Rüya Kaya, İlhami̇ Gülçi̇n
Turkish Journal of Chemistry
Cancer is a disease characterized by the continuous growth of cells without adherence to the rules that healthy normal cells obey. Carbonic anhydrase I and II (CA I and CA II) inhibitors are used for the treatment of some diseases. The available drugs in the market have limitations or side effects, which bring about the need to develop new drug candidate compound(s) to overcome the problems at issue. In this study, new pyrazole-sulphonamide hybrid compounds 4-[5-(1,3-benzodioxol-5-yl)-3-aryl-4,5-dihydro-1Hpyrazol- 1-yl]benzenesulphonamides (4a - 4j) were designed to discover new drug candidate compounds. The compounds 4a - 4j were synthesized and their chemical structures were …
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 …
Carbonic Anhydrase From Nicotiana Tabacum Leaves, Nazan Demi̇r, Yaşar Demi̇r
Carbonic Anhydrase From Nicotiana Tabacum Leaves, Nazan Demi̇r, Yaşar Demi̇r
Turkish Journal of Chemistry
In this study, carbonic anhydrase (CA: carbonate hydrolyase; E.C.4.2.1.1) was purified from adult {\it Nicotiana tabacum} leaves and studied biochemically. The enzyme was purified twice times by using (NH$_4)_2SO_4 precipation and DEAE-cellulose column chromatography, and its activity was determined for two different substrates (CO_2 and p-nitrophenyl acetate). The enzyme obtained from the ion exchange column was purified 40.7 fold and the purity was controlled by 3\%-10\% discontinuous SDS-PAGE. The pH of the purified enzyme varied between 6.0 and 7.2, the optimum being 6.9. V_{max} and K_m values were calculated with p-nitrophenyl acetate (0.1524 mM, 0.5446 mM, respectively) as substrate. The …