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Full-Text Articles in Physical Sciences and Mathematics
Design, Synthesis, And Enzyme Inhibition Evaluation Of Some Novel Mono- And Di-O-Ss-D-Glycopyranosyl Chalcone Analogues With Molecular Docking Studies, Gonca Çeli̇k, Gi̇zem Tatar Yilmaz, Hüseyi̇n Şahi̇n, Burak Barut, Nuretti̇n Yayli
Design, Synthesis, And Enzyme Inhibition Evaluation Of Some Novel Mono- And Di-O-Ss-D-Glycopyranosyl Chalcone Analogues With Molecular Docking Studies, Gonca Çeli̇k, Gi̇zem Tatar Yilmaz, Hüseyi̇n Şahi̇n, Burak Barut, Nuretti̇n Yayli
Turkish Journal of Chemistry
In this study, some novel mono- and di-O-β-D-glycopyranosyl chalcone analogs were designed, synthesized, and characterized. The chalcone derivatives were synthesized with good yields by base-catalyzed Claisen-Schmidt condensation in EtOH solution. Then these chalcones were reacted with TAGBr (2,3,4,6-tetra-O-acetyl-μ-D-glucopyranosylbromide) in dry acetone under the anhydrous condition at 0-5 °C. Deacylated was carried out by the Zemplen's method with NaOCH3 in dry methanol results in substituted chalcone-O-glycosides (mono- and di-O-β-D-glycopyranosyl chalcone analogs). The chemical structures of all synthesized compounds were elucidated based on IR, NMR spectral data, and mass spectrometry. Further, the compounds (7a-c, 8a-c, 12a-c, 16a-c, and 17a-c) …
Comprehensive Evaluation Of Reseda Lutea L. (Wild Mignonette) And 7 Isolated Flavonol Glycosides: Determination Of Antioxidant Activity, Anti-Alzheimer, Antidiabetic And Cytotoxic Effects With In Vitro And In Silico Methods, Hati̇ce Kiziltaş
Turkish Journal of Chemistry
In this study, anticholinergic, antidiabetic, antioxidant and cytotoxic activities of Reseda lutea L. (R. lutea) were determined. Ethanol extracts of R. lutea (EERL) and water extract of R. lutea (WERL) were prepared for biochemical analysis. The antioxidant capacities of EERL and WERL were evaluated with 6 different methods. In addition, acetylcholinesterase (AChE), α-amylase and α-glycosidase enzyme inhibition by EERL were measured. According to the results, EERL exhibited high inhibition effects against α-amylase, α-glycosidase and AChE enzymes. The IC50 values of EERL against AChE (2.21 μg/mL), α-glycosidase (1.38 μg/mL), and α-amylase (0.11 μg/mL) were determined. Also, high cytotoxic effect of EERL …
Synthesis Of Hydroxy Benzoin/Benzil Analogs And Investigation Of Their Antioxidant,Antimicrobial, Enzyme Inhibition, And Cytotoxic Activities, Nuretti̇n Yayli, Gözde Kiliç, Gonca Çeli̇k, Nuran Kahri̇man, Şeyda Kanbolat, Ari̇f Bozdeveci̇, Şengül Alpay Karaoğlu, Rezzan Ali̇yazicioğlu, Hasan Erdi̇nç Selli̇tepe, İnci̇ Seli̇n Doğan, Ali̇ Aydin
Synthesis Of Hydroxy Benzoin/Benzil Analogs And Investigation Of Their Antioxidant,Antimicrobial, Enzyme Inhibition, And Cytotoxic Activities, Nuretti̇n Yayli, Gözde Kiliç, Gonca Çeli̇k, Nuran Kahri̇man, Şeyda Kanbolat, Ari̇f Bozdeveci̇, Şengül Alpay Karaoğlu, Rezzan Ali̇yazicioğlu, Hasan Erdi̇nç Selli̇tepe, İnci̇ Seli̇n Doğan, Ali̇ Aydin
Turkish Journal of Chemistry
In this study, hydroxy benzoin (1-7), benzil (8-14), and benzoin/benzil-O-β-D-glucosides (15-25) were synthesized to investigate their biological activities. An efficient method for synthesizing hydroxy benzoin compounds (1-7) was prepared from four different benzaldehydes using an ultrasonic bath. Then, antioxidant (FRAP, CUPRAC, and DPPH), antimicrobial (3 Gram (-), 4/6 Gram (+), one tuberculosis and one fungus), and enzyme inhibition (acetylcholinesterase, butyrylcholine esterase, tyrosinase, α-amylase, and α- glucosidase) for the all synthesized compounds (1-25) were evaluated. And also, four most active compounds (4, 12, 18a+b, and 25) from each group were evaluated to the human cervical cancer cell line (HeLa) and anticancer …
New Sandwich-Type Polymeric Potassium-Dicyanoargentate(I) Complex: Synthesis, Characterization And Enzymatic Activity, Nesri̇n Korkmaz
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 …
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 …
Biological Evaluation And Synthesis Of New Pyrimidine-2(1h)-Ol/-Thiol Derivatives Derived From Chalcones Using The Solid Phase Microwave Method, Seda Fandakli, Nuran Kahri̇man, Tayyi̇be Beyza Yücel, Şengül Alpay Karaoğlu, Nuretti̇n Yayli
Biological Evaluation And Synthesis Of New Pyrimidine-2(1h)-Ol/-Thiol Derivatives Derived From Chalcones Using The Solid Phase Microwave Method, Seda Fandakli, Nuran Kahri̇man, Tayyi̇be Beyza Yücel, Şengül Alpay Karaoğlu, Nuretti̇n Yayli
Turkish Journal of Chemistry
Twenty-five new hydroxy- and methoxy-substituted 4,6-diarylpyrimidin-2(1H)-ol (20-34) and 4,6-diarylpyri\-midine-2(1H)-thiol derivatives (35-44) were synthesized from the reaction of the corresponding 1,3-diaryl-2-propene-1-one compounds (1-19) with urea or thiourea using the solid-phase microwave method. All the new synthetic compounds (20-44) were evaluated with regard to their $\alpha $-glucosidase activity. However, only compounds 22-25, 27,31,34, 35,37, and 40 exhibited a greater inhibitory effect than standard acarbose. The IC$_{50}$ values of the active compounds ranged between 2.36 and 13.34 $\mu $M. The 25 new compounds were also screened for their in vitro pancreatic lipase activity and compounds 20-27and 35-39 were found to be active. Of …
Synthesis And Mao Inhibitory Activity Of Novel Thiazole-Hydrazones, Özlem Atli, Yusuf Özkay
Synthesis And Mao Inhibitory Activity Of Novel Thiazole-Hydrazones, Özlem Atli, Yusuf Özkay
Turkish Journal of Chemistry
A series of new thiazole-hydrazones 3a-3n were synthesized, characterized, and screened for their $h$MAO-A and $h$MAO-B inhibitory activity by an in vitro fluorometric method. Selectivity indexes (SIs) were expressed as IC$_{50}$ (MAO-A) / IC$_{50}$ (MAO-B). Compound 3f showed promising $h$MAO-A inhibition with an IC$_{50}$ value of 1.20 $\mu $M and displayed a very significant SI of 0.04 towards $h$MAO-A. The mechanism of $h$MAO-A inhibition was investigated by enzyme kinetics using Lineweaver--Burk graphics. Compound 3f was further screened for its cytotoxicity by using a healthy NIH/3T3 mouse embryonic fibroblast cell line (ATCC CRL1658) and was evaluated as nontoxic at its effective …
Properties And Some In Vitro Studies Of 6-Phosphogluconate Dehydrogenase Purified From The Liver Of Chalcalburnus Tarichi, The Only Fish Living In Lake Van's Highly Alkaline Water (Ph 9.8), Muhammet Güler, Vedat Türkoğlu, Mehmet Riza Kivanç
Properties And Some In Vitro Studies Of 6-Phosphogluconate Dehydrogenase Purified From The Liver Of Chalcalburnus Tarichi, The Only Fish Living In Lake Van's Highly Alkaline Water (Ph 9.8), Muhammet Güler, Vedat Türkoğlu, Mehmet Riza Kivanç
Turkish Journal of Chemistry
In this study, some enzymology parameters and some antibiotics affecting the enzyme activity of 6-phosphogluconate dehydrogenase (6PGD) extracted from t the livers of fish from Lake Van (\textit{Chalcalburnus tarichi}) were investigated because it is an important enzyme-producing NADPH, a reductive power, protecting the cell against the oxidative agents by producing reduced glutathione. The crude enzyme solution was obtained by using the affinity chromatography method. The native molecular weight of the enzyme is $\sim $90,000 $\pm $ 3000 Da and it is composed of two subunits with identical molecular weights of $\sim $46,000 Da as exhibited on sodium dodecyl sulfate-polyacrylamide gel …
Synthesis, Biological Evaluation, And Molecular Docking Of N'-(Aryl/Alkylsulfonyl)-1-(Phenylsulfonyl) Piperidine-4-Carbohydrazide Derivatives, Hira Khalid, Aziz Ur Rehman, Muhammad Athar Abbasi, Rashad Hussain, Khalid Mohammad Khan, Muhammad Ashraf, Syeda Abida Ejaz, Muhammad Qaiser Fatmi
Synthesis, Biological Evaluation, And Molecular Docking Of N'-(Aryl/Alkylsulfonyl)-1-(Phenylsulfonyl) Piperidine-4-Carbohydrazide Derivatives, Hira Khalid, Aziz Ur Rehman, Muhammad Athar Abbasi, Rashad Hussain, Khalid Mohammad Khan, Muhammad Ashraf, Syeda Abida Ejaz, Muhammad Qaiser Fatmi
Turkish Journal of Chemistry
A series of new N'-[(alkyl/aryl)sulfonyl]-1-(phenylsulfonyl)piperidine-4-carbohydrazide derivatives were synthesized. Starting from ethyl piperidine-4-carboxylate (a), first ethyl 1-(phenylsulfonyl)piperidine-4-carboxylate (1), second 1-(phenylsulfonyl)piperidine-4-carbohydrazide (2), and finally N'-[(alkyl/aryl)sulfonyl]-1-(phenylsulfonyl)piperidine-4-carbohydrazides (4a--n) were synthesized by reacting 2 with alkyl/aryl sulfonyl chlorides (3a--n). The structures of the synthesized compounds were characterized by IR, ^1H-NMR, and EI-MS spectra and all were screened in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzyme inhibition activities. Molecular docking was accomplished for these compounds to examine their binding interactions with AChE and BChE human proteins. The strategy we applied for this purpose was a direct receptor-based approach. The binding modes of the inhibitors …
Rosmarinic Acid: A Potent Carbonic Anhydrase Isoenzymes Inhibitor, Meryem Topal, İlhami̇ Gülçi̇n
Rosmarinic Acid: A Potent Carbonic Anhydrase Isoenzymes Inhibitor, Meryem Topal, İlhami̇ Gülçi̇n
Turkish Journal of Chemistry
Rosmarinic acid is a water-soluble ester of caffeic acid and 3,4-dihydroxyphenyllactic acids, and is mainly found in plant species including Boraginaceae and Lamiaceae. In this research, we determined the inhibition property of rosmarinic acid on carbonic anhydrase isoenzymes I and II (hCA I and II) purified from human erythrocytes by using Sepharose-4B affinity column chromatography. hCA I and II isoenzymes were obtained with a yield of 57.9% and 67.2% and 76.5- and 509.3-fold purification of each isoenzyme, respectively. In order to show the purity of the isoenzymes, SDS-PAGE was performed and one band was observed. In vitro inhibition of both …
Synthesis And Evaluation Of Enzyme Inhibitory Potential Of Some Derivatives Of Scopolamine, Durre Shahwar, Muhammad Asam Raza, Tania Khan
Synthesis And Evaluation Of Enzyme Inhibitory Potential Of Some Derivatives Of Scopolamine, Durre Shahwar, Muhammad Asam Raza, Tania Khan
Turkish Journal of Chemistry
This study was designed to synthesize and evaluate derivatives of scopolamine (1) as acetylcholine esterase and protease inhibitors. Scopolamine (1) was extracted from the aerial parts of Datura innoxia through bioassay guided fractionation. Five different derivatives of scopolamine (1) were synthesized, and identified through spectroscopic studies. Their acetylcholine esterase (AChE) and trypsin inhibitory potentials were determined through standard protocols and evaluated from the perspective of structure-activity relationship. The synthesized scopolamine derivatives (2-6) showed remarkable AChE inhibitory activity, except for scopoline (6). The results showed higher enzyme inhibition potential of the synthesized compounds (2-5) as compared to scopolamine (1). Maximum inhibition …
A New Ursane-Type Triterpenoid From Salvia Santolinifolia, Zaher Ahmad, Sajid Mehmood, Rehana Ifzal, Abdul Malik, Nighat Afza, Mohammad Ashraf, Erum Jahan
A New Ursane-Type Triterpenoid From Salvia Santolinifolia, Zaher Ahmad, Sajid Mehmood, Rehana Ifzal, Abdul Malik, Nighat Afza, Mohammad Ashraf, Erum Jahan
Turkish Journal of Chemistry
Santolinoic acid (1), a new ursane-type triterpene was isolated from the chloroform soluble fraction of Salvia santolinifolia. Its structure was established as 2\alpha, 3\beta, 9\alpha-trihydroxyurs-12-en-28-oic acid on the basis of spectroscopic analysis, including high resolution mass spectroscopy, and 1- and 2-dimensional NMR techniques. The compound (1) showed inhibitory activity against the enzymes acetylcholinesterase and butyrylcholinesterase.