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ZENGİN KURT, BELMA

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ZENGİN KURT
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Author: Sonmez, Fatih × Author: Kurt, BELMA ×

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    Two New Co(II) Complexes of Picolinate: Synthesis, Crystal Structure, Spectral Characterization, -Glucosidase nhibition and TD/DFT Study
    (2019-07-01) Alturk, Suemeyye; Avci, Davut; Kurt, BELMA; Tamer, Omer; Basoglu, Adil; Sonmez, Fatih; Atalay, Yusuf; Dege, Necmi; ZENGİN KURT, BELMA
    Co(II) complexes of 2-picolinic acid (picH) and 6-methylpyridine-2-carboxylic acid (6-MepicH) {[Co(pic)(2)2H(2)O], (1), [Co(6-Mepic)(pic)2H(2)O], (2)} were obtained and their structural and spectroscopic properties were investigated by XRD, FT-IR and UV-Vis spectroscopic techniques. The measurement of -glucosidase inhibition of the synthesized complex 2 was fulfilled by IC50 values. In order to provide further explanations about the electronic spectral properties, TD-DFT calculations in ethanol solvent and gas phase were carried out. HSEh1PBE/6-311G(d,p) level has been used to calculate the nonlinear optics (NLO) parameters and frontier molecular orbital (FMO) energies. The experimental refractive indexes and optical band gap energies for the Co(II) complexes have been obtained using FT-IR and UV-Vis spectra, respectively. Lastly, the molecular docking study of Co(II) complexes was carried out in order to demonstrate interactions between the synthesized complexes and target protein (the template structure S. cerevisiae isomaltase).
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    Synthesis, antioxidant and carbonic anhydrase I and II inhibitory activities of novel sulphonamide-substituted coumarylthiazole derivatives
    (2016-01-01) Kurt, BELMA; Sonmez, Fatih; Bilen, Cigdem; Ergun, Adem; Gencer, Nahit; Arslan, Oktay; Kucukislamoglu, Mustafa; ZENGİN KURT, BELMA
    New secondary benzenesulphonamide-substituted coumarylthiazole derivatives were synthesized and their inhibitory effects on purified carbonic anhydrase I and II were evaluated using CO2 as a substrate. The result showed that all the synthesized compounds exhibited inhibitory activity on both hCA I and hCA II with N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl) naphthalene-2-sulphonamide (5f, IC50 value of 5.63 and 8.48 mu M, against hCA I and hCA II, respectively) as the strongest inhibitor revealed from this study. Structure-activity relationship revealed that the inhibitory activity of the synthesized compounds is related to the type of the halogen and bulky substituent on the phenyl ring. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were assayed. 4-methoxy-N-(4-(2-oxo-2H-chromen-3-yl) thiazol-2-yl) benzenesulphonamide (5e) exhibited the strongest ABTS and CUPRAC activity with IC50 value of 48.83 mu M and A(0.50) value of 23.29 mu M ,
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    Three novel Cu(II), Cd(II) and Cr(III) complexes of 6-Methylpyridine-2-carboxylic acid with thiocyanate: Synthesis, crystal structures, DFT calculations, molecular docking and alpha-Glucosidase inhibition studies
    (2018-12-13) Avci, Davut; Alturk, Sumeyye; Sonmez, Fatih; Tamer, Omer; Basoglu, Adil; Atalay, Yusuf; Kurt, BELMA; Dege, Necmi; ZENGİN KURT, BELMA
    Novel complexes of 6-methylpyridine-2-carboxylic acid and thiocyanate ([Cu(NCS)(6-mpa)(2)], (1); [Cd(NCS)(6-mpa)](n), (2); [Cr(NCS)(6-mpa)(2)center dot H2O], (3)} were synthesized, and their structures were characterized by XRD analysis, FT-IR and UV-Vis spectroscopic techniques. The inhibitory activities of the synthesized complexes (1-3) on alpha-glucosidase were determined by using genistein reference compound. Furthermore, the optimized geometry and vibrational harmonic frequencies for the complexes 1-3 were obtained by DFT/HSEh1PBE/6-311G(d,p)/LanL2DZ level. Electronic spectral properties were examined by using TD-DFT/FISEh1PBE/6-311G(d,p)/LanL2DZ level with CPCM model. Additionally, major contributions to the electronic transitions were determined via Swizard program. The refractive index, linear optical and non-nonlinear optical parameters of the complexes 1-3 were investigated at HSEh1PBE/6 -311G(d,p) level. The docking studies of the complexes 1-3 to the binding site of the target protein (the template structure S. cerevisiae isomaltase are fulfilled. Lastly, natural bond orbital analysis was used to investigate inter- and intra-molecular bonding and interaction among bonds. (C) 2018 Elsevier Ltd. All rights reserved.
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    In vitro inhibition effects on erythrocyte carbonic anhydrase I and II and structure-activity relationships of cumarylthiazole derivatives
    (2016-09-01) Kurt, BELMA; Sonmez, Fatih; GÖKÇE, Başak; Ergun, Adem; Gencer, Nahit; Demir, Taki; Arslan, Oktay; Kucukislamoglu, Mustafa; ZENGİN KURT, BELMA
    Coumarin and heterocyclic compounds incorporating urea have clinical applications as antiepileptics, diuretics, and antiglaucoma agents due to their carbonic anhydrase inhibitory properties. We investigated inhibition of carbonic anhydrase I and II with a series of coumarylthiazole derivatives containing urea/thiourea groups. All the investigated compounds exhibited inhibitory activity on both hCA I and hCA II, with 1-(3-chlorophenyl)-3-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)urea being the strongest inhibitor. Structure-activity relationship study showed that most of urea derivatives were more inhibiting for hCA I and hCA II than thiourea derivatives. The electron-withdrawing groups at the phenyl ring increased the inhibitory activity compared to electron-donating groups.
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    Optimization of ultrasound-assisted extraction of total phenolic contents and antioxidant activity using response surface methodology from jujube leaves (Ziziphus jujuba) and evaluation of anticholinesterase inhibitory activity
    (2019-03-01) Zemouri-Alioui, Salima; Bey, Mostapha Bachir; Kurt, BELMA; Sonmez, Fatih; ZENGİN KURT, BELMA
    An ultrasound-assisted procedure for the extraction of phenolics (TPC) and antioxidant activity (AA) from jujube leaves have been investigated using response surface methodology (RSM). The Box-Behnken design was used to investigate the effects of three independent variables, solvent concentration (methanol/water; 40-100%), ultrasound-intensity (20-100%), and extraction time (3-15min) on the responses. The optimal extraction conditions were 64.20% methanol, 73.60% ultrasound intensity, and 13.27min. Under optimal conditions, the corresponding experimental values for TPC and AA were 6098.14mg GAE/100g DMand 4010.63mg AAE/100g DM. The experimental values were in close agreement with those predicted values within a 99% confidence level, thus indicating the suitability of the model and the success of RSM in optimizing the ultrasound assisted extraction of TPC and AA of jujube leaves. The results showed that optimized jujube leaves extract exhibited inhibitory effects on both acetylcholinesterase and butyrylcholinesterase with IC50 of 62.30 +/- 2.54 and 147.00 +/- 2.31 mu g/mL, respectively.
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    Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer-s disease
    (2015-09-18) Kurt, BELMA; Gazioglu, IŞIL; BASILE, Livia; Sonmez, Fatih; GINEX, Tiziana; Kucukislamoglu, Mustafa; GUCCIONE, Salvatore; ZENGİN KURT, BELMA; GAZİOĞLU, IŞIL
    New benzofuranylthiazole derivatives containing the aryl urea moiety were synthesized and evaluated in vitro as dual acetylcholinesterase (AChE)-butyrylcholinesterase (BuChE) inhibitors. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were assayed. The result showed that all the synthesized compounds exhibited inhibitory activity on both AChE and BuChE with 1-(4-(5-bromobenzofuran-2-yl)thiazol-2-yl)-3-(2fluorophenyl)urea (e25, IC50 value of 3.85 mu M) and 1-(4-iodophenyl)-3-(4-(5-nitrobenzofuran-2-yl) thiazol-2-yl)urea (e38, IC50 value of 2.03 mu M) as the strongest inhibitors against AChE and BuChE, respectively. Compound e38 was 8.5-fold more potent than galanthamine. The selectivity index of e25 and e38 was 2.40 and 0.37 against AChE and BuChE, respectively. Compound e2, e4 and ell (IC50 = 0.2, 0.5 and 1.13 mu M, respectively) showed a better ABTS cation radical scavenging ability than the standard quercetin (IC50 = 1.18 AM). Best poses of compounds e38 on BuChE and e25 on AChE indicate that the thiazole ring and the amidic moiety are important sites of interaction with both ChEs. In addition, the benzofuran ring and phenyl ring are anchored to the side chains of both enzymes by pi-pi(pi-pi) interactions. (C) 2015 Elsevier Masson SAS. All rights reserved.
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    Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives
    (2015-04-01) Kurt, BELMA; Gazioglu, IŞIL; Sonmez, Fatih; Kucukislamoglu, Mustafa; ZENGİN KURT, BELMA; GAZİOĞLU, IŞIL
    A newly series of coumarylthiazole derivatives containing aryl urea/thiourea groups were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. The result showed that all the synthesized compounds exhibited inhibitory activity to both cholinesterases. Among them, 1-(4-(8-methoxy-2-oxo-2H-chromen-3-yl)thiazol-2-yl)-3-(4-chlorophenyl)thiourea (f8, IC50 = 4.58 mu M) was found to be the most active compound against AChE, and 1-(4-fluorophenyl)-3-(4-(6-nitro-2-oxo-2H-chromen-3-yl)thiazol-2-yl)urea (e31) exhibited the strongest inhibition against BuChE with IC50 value of 4.93 mu M, which was 3.5-fold more potent than that of galantamine. The selectivity of f8 and e31 were 2.64 and 0.04, respectively. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were investigated for antioxidant activity. Among them, f8, f4 and f6 (IC50 = 1.64, 1.82 and 2.69 mu M, respectively) showed significantly better ABTS cation radical scavenging ability than standard quercetin (IC50 = 15.49 mu M). (C) 2015 Elsevier Inc. All rights reserved.
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    Synthesis and biological evaluation of novel coumarin-chalcone derivatives containing urea moiety as potential anticancer agents
    (2020-01-01T00:00:00Z) Kurt, BELMA; Kandas, Nur Ozten; DAĞ, AYDAN; Sonmez, Fatih; Kucukislamoglu, Mustafa; ZENGİN KURT, BELMA; DAĞ, AYDAN
    The increasing interest on new drug discovery is constantly up to date as drugs do not increase survival adequately against increasing cancer cases worldwide. Based on the reported anticancer activity of coumarin, chalcone and urea derivatives, the present investigation dealt with the design and synthesis of coumarin derivatives bearing diversely substituted chalcone-urea moieties 5a-k. Through a structure-based molecular hybridization approach, a series of novel coumarin-chalcone derivatives containing urea moiety was synthesized and screened for their in vitro antiproliferative activities against the cancer cell lines (H4IIE and HepG2). In addition, the synthesized compounds were tested on a cell line that was not cancerous (CHO) and the damage, it could give to normal cells was determined. Among the synthesized compounds, 5k exhibited better inhibition of H4IIE compared to Sorafenib. 5j also showed better inhibition against HepG2 than Sorafenib. In particular, 5k induced H4IIE apoptosis, arrested cell cycle at the S phase. Therefore, 5k and 5j may be potent antitumor agents, representing a promising lead for further optimization. (C) 2017 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.