Person: KAYMAKÇIOĞLU, BEDİA
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KAYMAKÇIOĞLU
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BEDİA
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Publication Open Access Synthesis of some novel 1,3,4-oxadiazole derivatives and evaluation of their antimicrobial activity(2022-01-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., Kaya M., KARACA GENÇER H., KAYMAKÇIOĞLU B.Treatment for microbial infections still remains an important health problem for researchers around the world. Despite a broad range of antimicrobial drugs today, there are certain obstacles associated with the use of antimicrobial agents such as drug resistance and toxicity. Thus, medicinal chemists concentrate on designing novel antimicrobial drugs. In the search for new antimicrobial agents; 1,3,4-oxadiazole compounds have come forward due to their hydrolytic stability, good chemical and thermal stability. In the scope of this work, 2-(6-chloropyridin-3-yl)-5-(substitutedphenyl)-1,3,4-oxadiazole (4a-4i) were synthesizedusing 6-chloro-N\"-(substitutedbenzoyl)nicotinohydrazide (3a-3i). These compounds were screened for their antimicrobial activities against as gram-positive bacteria S. aureus, E. faecalis, as gram-negative bacteria E. coli, P. aeruginosa, as yeast C. parapsilosis, C. albicans, C. glabrata. Among the 1,3,4-oxadiazole compounds, 4h against E. faecalis and 4b, 4f and 4g against E. coli have been found to exhibit as much as potency chloramphenicol with MIC50 values of 62.50 mu g/mL.Publication Open Access Synthesis of novel pyrazoline derivatives and evaluation of their antimicrobial activity(2022-01-01) TOK, FATİH; GÜRBÜZ, BURÇAK; KAYMAKÇIOĞLU, BEDİA; TOK F., Doğan M. O. , GÜRBÜZ B., Koçyiğit-Kaymakçioğlu B.© 2022 Marmara University Press.In this study, new nine pyrazoline derivatives were synthesized from chalcone derivatives. The antimicrobial activity of nine pyrazoline derivatives to four standard bacterial strains (Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis) and four standard yeast strains (Candida albicans, Candida glabrata, Candida parapsilosis, Candida tropicalis) was investigated by the microdilution method for in accordance with the Clinical and Laboratory Standards Institute (CLSI) standard, and the Minimal Inhibitory Concentration (MIC) values of these derivatives were determined. Among these derivatives; compounds 7 and 8 against bacterial strains and compounds 2 and 3 against yeast strains exhibited good antimicrobial activity.Publication Open Access Design, synthesis, in silico ADMET studies and anticancer activity of some new pyrazoline and benzodioxole derivatives(2022-01-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., ERDOĞAN Ö., ÇEVİK Ö., KAYMAKÇIOĞLU B.A new series of 2-pyrazoline derivatives starting from substituted benzodioxole chalcones were designed and synthesized. IR and 1H NMR spectral data and elemental analysis were used to characterize the structures of the synthesized compounds. The cytotoxic activities on HeLa, MCF-7 cancer cell lines and NIH-3T3 for these compounds were tested by using MTT assay. Among the synthesized compounds 2d, 2j, 3j and 3n against MCF-7 cells, and 3c against HeLa exhibited significant cytotoxic activity with IC50 between 10.08 and 27.63 mu M. Compound 3f showed the most potent anticancer activity against both cancer cells with good selectivity (IC50 = 11.53 mu M on HeLa with SI = 81.75 and IC50 = 11.37 mu M on MCF-7 with SI = 82.90). Furthermore, in silico ADMET analyses were performed and the drug-likeness properties of the compounds were investigated.Publication Open Access N-Substituted Arylidene-3-(Methylsulfonyl)-2-Oxoimidazolidine-1-Carbohydrazide as Cholinesterase Inhibitors: Design, Synthesis, and Molecular Docking Study(2022-08-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., SAĞLIK B. N., ÖZKAY Y., KAPLANCIKLI Z. A., KAYMAKÇIOĞLU B.The development of new enzyme inhibitors in degenerative brain diseases has gained more attention. Enzyme inhibitors play an effective role in controlling central nervous system diseases. For this purpose, a novel series of hydrazone derivatives containing imidazolidine ring aimed against Alzheimer\"s disease (AD), have been designed and synthesized. The acetylcholinesterase (AChE) enzyme inhibitory activity of these compounds was investigated. The structures of the compounds were determined by IR, H-1 and C-13-NMR and mass spectroscopic methods. Inhibition studies on the cholinesterase (ChE) enzymes and beta-amyloid plaque inhibition test of the compounds were performed. Based on the experimental results, compound 3j bearing dimethoxy substituent on the aromatic ring like donepezil exhibited the most AChE inhibitory activity with the IC50 values of 0.023 +/- 0.001 mu M. Owing to obtained biological activity and molecular docking study results, it is thought that the most active compound 3j may play a role in both symptomatic and palliative treatment of AD.Publication Open Access Synthesis of novel thiosemicarbazone derivatives as antidiabetic agent with enzyme kinetic studies and antioxidant activity(2022-01-01) KAYMAKÇIOĞLU, BEDİA; TOK, FATİH; TOK F., KÜÇÜKAL B., BALTAŞ N., Yilmaz G. T., KAYMAKÇIOĞLU B.Novel thiosemicarbazone derivatives were synthesized via condensation reactions between the corresponding thiosemicarbazides and 4-(methylsulfonyl)acetophenone. The chemical structures of all compounds were elucidated by infrared (IR), H-1-NMR and C-13-NMR spectroscopy and mass spectrometry. Antioxidant studies of all compounds were performed by using CUPRAC, FRAP, DPPH methods. 2-{1-[4-(Methylsulfonyl)phenyl]ethylidene}-N-phenylhydrazinecarbothioamide (1) possessed good antioxidant activity with an SC50 value of 15.70 mu M which also is higher than standard drug, ascorbic acid. All compounds were evaluated for their antidiabetic properties as alpha-glycosidase and alpha-amylase inhibitors. Compound 1 was found to be the most active compound against alpha-glucosidase and alpha-amylase with IC50 values of 1.58 mu M and 3.24 mu M, respectively. The enzyme kinetic studies demonstrated that compound 1 has a competitive mode of binding. Furthermore, molecular docking studies have elucidated the binding mechanism at the molecular level by examining the molecular interactions between compound 1 and these enzymes.Publication Open Access Synthesis of phthalimide derivatives and their insecticidal activity against caribbean fruit fly, anastrepha suspensa (Loew)(2023-02-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., Yang X., Tabanca N., Koçyiğit-Kaymakçıoğlu B.In this study, thirteen phthalimide derivatives were designed and synthesized. All synthesized compounds were evaluated to determine their potential for inhibitory activities against females of the Caribbean fruit fly, Anastrepha suspensa (Loew) (Diptera: Tephritidae). These efforts led to the discovery of three compounds 4a, 4c, and 4d with potent insecticidal activity (LD50 range from 0.70 to 1.91 μg/fly). Among these compounds, 4a exhibited the highest inhibitory potency with 0.70 μg/fly. In addition, in silico models indicated that compound 4a is less toxic than phthalimide and other precursors. Therefore, our results suggest that 4a has strong potential as a candidate component for developing a novel environmentally friendly insecticide for control of pest fruit flies.Publication Open Access Design, synthesis, biological activity evaluation and in silico studies of new nicotinohydrazide derivatives as multi-targeted inhibitors for Alzheimer's disease(2022-10-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., SAĞLIK B. N., ÖZKAY Y., KAPLANCIKLI Z. A., KAYMAKÇIOĞLU B.A new series of 6-chloro-N\"-(substituted benzylidene)nicotinohydrazide were synthesized via condensation reactions between the corresponding hydrazides and aldehydes . All compounds were tested for their AChE and BuChE inhibitory activity. Compounds P5, P7, P9, P10 and P12 exhibited significant AChE inhibition potencies. Among them, compound P5 having para nitro substituent was found to be the most effective derivative against AChE with an IC50 value of 0.027 +/- 0.001 mu M. After that, the BACE-1 and beta-amyloid plaque inhibitory potencies of selected compounds P5, P7, P9, P10 and P12 were evaluated. Among them, compound P5 displayed the highest inhibition rate against the BACE-1 enzyme and beta-amyloid plaque. Molecular docking studies were carried out using both AChE and BACE-1 crystals to determine the compound\"s interactions with the enzyme\"s active sites. Furthermore, we evaluated the ADMET properties of compounds and their blood-brain barrier (BBB) permeation was also found to be high. (C) 2022 Elsevier B.V. All rights reserved.Publication Metadata only Therapeutic drug monitoring in pediatric patients treated with anti-tuberculosis medications by high performance liquid chromatography(2022-01-01) OKUYAN, BETÜL; TOK, FATİH; KARAKUŞ, SEVGİ; KAYMAKÇIOĞLU, BEDİA; SANCAR, MESUT; OKUYAN B., TOK F., KARAKUŞ S., Dalgiç N., ÇAKIR E., Midyat L., Koçyiğit-Kaymakçioğlu B., Berk U. E. , İZZETTİN F. V. , Rollas S., et al.© 2022 Marmara University Press.The aim of this study is to perform therapeutic drug monitoring for isoniazid (INH), rifampicin (RIF), and pyrazinamide (PZA) in pediatric tuberculosis patients. The study was carried out in 3 different training-research hospitals in Istanbul, Türkiye between 2011 and 2012. The pediatric patients (aged ≤14 years) who initiated the standard primary anti-tuberculosis therapy were included in this study. The serum samples were collected 3 hours after the first medication doses were given on the 5th day of treatment. Chromatographic experiments were performed on an Agilent 1100 High-Performance Liquid Chromatography (HPLC) system, and the separation was carried out on a Nova-Pak C18 (3.9x150 mm, 5 μm, Merck) analytical column. In this HPLC method, the gradient elusion delivered 3% to 40% (v/v) acetonitrile in phosphate buffer was used, and diode array detector. Twenty-three children (60.9% male) patients were included with a mean age of 111.70 ± 59.94 months. Plasma levels were measured sub-therapeutically for INH in 14, RIF in 10, and PZA in 5 patients, according to the normal range of adult patients. Maximum plasma concentrations after three hours were found between 0.53-14.02 mg/L for INH, 11.17-60.39 mg/L for PZA, 2.15-16.75 mg/L for RIF. In conclusion, this method has been successfully applied to simultaneously determine RIF, INH, and PZA plasma levels in pediatric tuberculosis patients. RIF and INH plasma levels were found to be lower in pediatric patients with tuberculosis compared to target range of adult patients.Publication Open Access Synthesis, Characterization, Molecular Docking Studies and Biological Evaluation of Some Novel 3,5-disubstituted-1-phenyl-4,5-dihydro-1H-pyrazole Derivatives(2024-01-01) TOK, FATİH; ÖZTÜRK, MEHMET; KAYMAKÇIOĞLU, BEDİA; TOK F., Bayrak İ. R., Karakaraman E., Soysal İ., Çakır C., Tuna K., Özgüven S. Y., Sıcak Y., Öztürk M., Koçyiğit-Kaymakçıoğlu B.In this study, some new pyrazoline derivatives bearing cyano or nitro groups were synthesized. The structures of the compounds were characterized by IR,1H-NMR,13C-NMR and elemental analysis data. The ABTS·+, DPPH·, CUPRAC and β-Carotene/linoleic acid assays were carried out to determine the antioxidant activity of the synthesized pyrazolines. Compound P14 showed higher antioxidant activity than the standard substance BHA with IC50 values of 1.71±0.31 µM and 0.29±0.04 µM in ABTS+ and β-carotene/linoleic acid assays, respectively. Compound P12 also exhibited higher antioxidant activities than BHA with an IC50 value of 0.36±0.14 µM in β-carotene/linoleic acid analysis. In activity studies of pyrazolines against cholinesterase (AChE and BChE), tyrosinase, α-amylase and α-glucosidase, compound P1 (IC50 = 39.51±3.80 µM) showed higher activity against α-amylase and compounds P5 and P12 displayed higher activity against α-glucosidase than acarbose with IC50 values of 14.09±0.62 and 83.26±2.57 µM, respectively. The drug-like properties such as Lipinski and Veber, bioavailability and toxicity risks of the synthesized compounds were also evaluated. The compounds were predicted to be compatible with Lipinski and Veber rules, have high bioavailability and low toxicity profiles. Moreover, molecular docking studies were performed to better understand the high activity of the compounds against a-amylase and a-glucosidase enzymes.Publication Metadata only Recent advances in the microwave and ultrasound-assisted synthesis of pyrazole scaffolds(2023-01-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., Koçyiğit-Kaymakçıoğlu B.Pyrazoles are well-known five-membered heterocyclic compounds and are found in a wide variety of synthetic and natural compounds. Compounds carrying pyrazole scaffolds exhibit a wide range of biological activities such as anticancer, antimicrobial, anticon-vulsant, antioxidant, analgesic and anti-inflammatory effects. Pharmaceuticals with many different activities in the pyrazole structure are currently on the market (e.g., celecoxib, lona-zolac, tepoxalin, rimonabant, pyrazofurin, epirizole). The pyrazole ring contains the N-N double bond, which is thought to have a key role in biological activity, and compounds with this bond are difficult to produce by organisms, so their relative abundance is very low in nature. For this reason, many studies have been carried out on this structure and it has been revealed that the structure has a unique effect spectrum. Microwave-assisted synthesis has opened up some new opportunities compared to conventional synthesis. It is possible to use less solvent and reduce processing time with microwave synthesis. In addition, better selectivity and thermal stability are provided by microwave synthesis. Ultrasound-assisted synthesis is often used to enhance conventional solvent extraction, while microwaves reveal bioactive compounds by heating without any solvent. In the traditional method of pyrazole syn-thesis; polar solvents, acidic and basic catalysts are needed in large quantities in the synthesis of pyrazole scaffolds. This review aims to summarize the recent advancements in the synthesis methods of a pyrazole ring with non-traditional methods. Therefore this article will provide readers with a new perspective on the synthesis of pyrazole scaffolds as an environmentally friendly alternative.