Person: KAYMAKÇIOĞLU, BEDİA
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KAYMAKÇIOĞLU
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BEDİA
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Publication Open Access Synthesis and anticonvulsant activity of some 2-pyrazolines derived from chalcones(ELSEVIER SCIENCE BV, 2017-05) KAYMAKÇIOĞLU, BEDİA; Beyhan, Nagihan; Kocyigit-Kaymakcioglu, Bedia; Gumru, Salih; Aricioglu, FeyzaSynthesis of chalcones (1,3-diarylprop-2-en-1-ones) and 2-pyrazoline derivatives has been an active field of research due to their established pharmacological effects. In this study, a series of chalcones were prepared with methyl aryl ketones and substituted aldehydes in the presence of sodium hydroxide and methanol through Claisen-Schmidt condensation. 3,5-Disubstituted4,5-dihydro-1H-pyrazole-1-carbothioamides were synthesized by refluxing selected chalcones and thiosemicarbazide in alkaline medium. Similarly N-3,5-trisubstituted-4,5-dihydro-1H-pyrazole-1-carboxamides were synthesized by refluxing selected chalcones with N-(4-chlorophenyl) semicarbazide in alkaline medium. Structures of the synthesized compounds were confirmed by elemental analysis and spectral (UV, IR, H-1 NMR, C-13 NMR, and mass) data, which were in line with the proposed structures. All compounds were tested for their anticonvulsant activity using pentylenetetrazole induced seizure (PTZ) and maximal electroshock seizure (MES) tests in mice at a dose level of 50 mg/kg. Among the 2-pyrazoline-1-carbothioamide derivatives, 5-(2,6-dichlorophenyl)-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (2e) reduced grade-5 seizure activity and also increased survival rate in PTZ test. In MES test, 5-(4-methoxyphenyl)-3-[4-(methylsulphonyl) phenyl]-4,5-dihydro-1H-pyrazole-1-carbothioamide(2g) has not only decreased seizure severity, but also increased survival rate. Among the 2-pyrazoline-1-carboxamide derivatives, 3-(5-bromothiophen-2-yl)-N-(4-chlorophenyl)-5-(2,6-dichlorophenyl)-4,5-dihydro-1H-pyrazole-1-carboxamide (3d) having 5-bromothiophen and 2,6-dichlorophenyl moieties and N-(4-chlorophenyl)-5-(2,6-dichloro-phenyl)-3-(5-chlorothiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carboxamide (3e) having 5-chlorothiophen and 2,6-dichlorophenyl moieties showed remarkable activities in PTZ test. Among all tested derivatives, compound 3d was found to be the most active one and reduced grade-5 seizure severity and also increased survival rate. (C) 2013 Production and hosting by Elsevier B.V. on behalf of King Saud University.Publication Metadata only Synthesis and biological evaluation of new pyrazolone Schiff bases as monoamine oxidase and cholinesterase inhibitors(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2019) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Kocyigit-Kaymakcioglu, Bedia; Saglik, Begum Nurpelin; Levent, Serkan; Ozkay, Yusuf; Kaplancikli, Zafer AsimIn the current work, Schiff base derivatives of antipyrine were synthesized. The chemical characterization of the compounds was confirmed using IR, H-1 NMR, C-13 NMR and mass spectroscopies. The inhibitory potency of synthesized compounds was investigated towards acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and monoamine oxidases A and B (MAO-A and MAO-B) enzymes. Some of the compounds displayed significant inhibitory activity against AChE and MAO-B enzymes, respectively. According to AChE enzyme inhibition assay, compounds 3e and 3g were found as the most potent derivatives with IC50 values of 0.285 mu M and 0.057 mu M, respectively. Also, compounds 3a (IC50 = 0.114 mu M), 3h (IC50 = 0.049 mu M), and 3i (IC50 = 0.054 mu M) were the most active derivatives against MAO-B enzyme activity. So as to understand inhibition type, enzyme kinetics studies were carried out. Furthermore, molecular docking studies were performed to define and evaluate the interaction mechanism between compounds 3g and 3h and related enzymes. ADME (Absorption, Distribution, Metabolism, and Excretion) and BBB (Blood, Brain, Barier) permeability predictions were applied to estimate pharmacokinetic profiles of synthesized compounds.Publication Metadata only Design, synthesis, biological evaluation and molecular docking of novel molecules to PARP-1 enzyme(SCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK, 2019) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Kocyigit-Kaumakcioglu, Bedia; Ilhan, Recep; Yilmaz, Sinem; Ballar-Kirmizibayrak, Petek; Taskim-Tok, TugbaPoly (ADP-ribose) polymerase (PARP) enzyme catalyzes the transfer of ADP-ribose into target proteins. Therefore, PARP is responsible for DNA repair, cell proliferation, and cell death. In this study, potential PARP enzyme inhibitors were designed and synthesized. The synthesized compounds were elucidated by Fourier-transform infrared spectroscopy, H-1 NMR, C-13 NMR, heteronuclear single-quantum correlation, and mass spectrometry, and their purity was checked via thin-layer chromatography, high-performance liquid chromatography, and elemental analysis. A total of 63 newly synthesized compounds were screened in terms of PARP inhibition by cellular PARylation assay in the HeLa cell line. It was found that 19 compounds significantly inhibited the H2O2-induced cellular PARylation. The chemosensitizer effect of these compounds in cancer cells treated with doxorubicin (doxo) was investigated. It was found that the combination of potent PARP inhibitors with doxo potentiated a cytotoxic effect, similar to that of olaparib. The results of the molecular docking and absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis revealed that compound 60 might be classified as a potential PARP inhibitor candidate. Taken together, all of the results suggested that carbohydrazide derivatives could be a promising lead for the treatment for cancer disorders.Publication Metadata only Discovery and structure activity relationships of 2-pyrazolines derived from chalcones from a pest management perspective(SPRINGER BIRKHAUSER, 2015) KAYMAKÇIOĞLU, BEDİA; Kocyigit-Kaymakcioglu, Bedia; Beyhan, Nagihan; Tabanca, Nurhayat; Ali, Abbas; Wedge, David E.; Duke, Stephen O.; Bernier, Ulrich R.; Khan, Ikhlas A.Synthesis of chalcones and 2-pyrazoline derivatives has been an active field of research due to the established pharmacological effects of these compounds. In this study, a series of chalcone (1a-i), 2-pyrazoline-1-carbothioamides (2a-i), and 2-pyrazoline-1-carboxamide derivatives (3a-g) were synthesized and screened for their potential pesticide activities. The proposed structures of all the synthesized compounds were confirmed using the elemental analysis, UV, IR, H-1-NMR, and mass spectroscopy. Among the total of 25 tested compounds, compounds 1g and 2a and 2e with Biting Deterrence Index (BDI) values of 0.85, 0.83, and 0.8, respectively, at 25 nmol/cm(2) showed the highest biting deterrent activity against Aedes aegypti, which was comparable to N,N-diethyl-3-methylbenzamide (DEET). Compounds 1g, 2a and 2e were subsequently tested in human-based repellent bioassays, and they showed MED (minimum effective dose) values of 0.375, 0.094, and 0.375 mg/cm(2), respectively. Compound 1e was the most toxic compound (LC50 = 2.58 ppm), followed by 1f (LC50 = 5.69 ppm) and 2g (LC50 = 15.14 ppm), against 1-day-old Ae. aegypti larvae. Compounds 1f and 2h 1f and 2h showed the greatest growth inhibition against Colletotrichum gloeosporioides (97.6 and 98.5 %, respectively) at the lowest dose (0.3 mu M), which was greater antifungal activity than with standard commercial fungicides captan and azoxystrobin. Compounds 2d, 2g and 2h produced 79.5, 98.3, and 82.3 % growth inhibition, respectively, at 30.0 mu M against Botrytis cinerea, which was similar to captan in the antifungal activity. The active fungicidal compounds (2d, 2g, and 2h) were weaky phytotoxic, with little or no phytotoxicity at concentrations that were fungitoxic. Compound 2h stimulated the growth of Lemma paucicostata at concentrations that are fungitoxic to several plant pathogens.Publication Metadata only Synthesis and Anticancer Activity of New Hydrazide-hydrazoncs and Their Pd(II) Complexes(BENTHAM SCIENCE PUBL LTD, 2019) KAYMAKÇIOĞLU, BEDİA; Kocyigit-Kaymakcioglu, Bedia; Yazici, Senem Sinem; Tok, Fatih; Dikmen, Miris; Engur, Selin; Oruc-Emre, Emine Elcin; Iyidogan, AysegulBackground: Hydrazones, one of the important classes of organic molecules, are pharmaceutical agents comprising -CO-NH-N=CH- group in the structure therefore and exhibiting significant biological activity. Methods: 5-Chloro-N'-[(substituted)methylidene] pyrazine-2-carbohydrazide (3a-g) and their Pd(II) complexes (4a-h) were synthesized and investigated in vitro anticancer activity on A549, Caco2 cancer and normal 3T3 fibroblast cell lines, using the MTT assay. Results: Anticancer activity screening results revealed that some compounds showed remarkable cytotoxic effect. Among them, 5-chloro-N'-[(4-hydroxyphenyl)methylidene] pyrazine-2-carbohydrazide (3c) displayed higher cytotoxic activity against A549 cancer cell line than the reference drug cisplatin. Conclusion: Compound 3c showed high cytotoxic activity against A549 cancer cell line but it showed low cytotoxic effect against normal 3T3 fibroblast cell line. Antiproliferative and antimetastatic effects of 3c were determined by the real-time monitoring of cell proliferative system (RTCA DP). The cell proliferation, metastatic and invasive activities of A549 cells were decreased due to increased concentration of 3c.Publication Open Access Antiproliferative activity of some tautomeric hydrazones derived from chalcones(MARMARA UNIV, FAC PHARMACY, 2016-02-02) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Beyhan, Nagihan; Erzurumlu, Yalcin; Ilhan, Recep; Ballar, Petek; Kocyigit-Kaymakcioglu, BediaA new series of hydrazones synthesized from chalcones. Synthesized compounds have been characterized by IR, H-1-NMR and elemental analysis. Antiproliferative activity of compounds was investigated on Hela, A549, MCF7, HCC1937, MRC5 cells. All compounds exhibited cytotoxicity. Especially compounds 1b, 1c, 1f and 1i having 4-metylsulfonyl phenyl showed higher cytotoxicity against all of the cell lines compared to reference drug doxorubicin with low value of IC50=5,56-21,93 mu M. The most active compounds 1b, 1c, 1f and 1i were analyzed for their effect on autophagic processes. HCC1937 cells were treated with these compounds at IC50 concentration for 24 hours. An immunoblotting assay was performed to analysis autophagy markers and total polyubiquitinated protein levels. Compounds 1b, 1c, 1f and 1i significantly increased the conversion of LC3-I to LC3-II at IC50 concentration. None of the tested compounds changed the level of total polyubiquitinated proteins.Publication Metadata only Antituberculosis activity of hydrazones derived from 4-fluorobenzoic acid hydrazide(SPRINGER BIRKHAUSER, 2009) KAYMAKÇIOĞLU, BEDİA; Kocyigit-Kaymakcioglu, Bedia; Oruc-Emre, Emine Elcin; Unsalan, Seda; Rollas, SevimA series of substitututed methylene/ethylene 4-fluorophenylhydrazide derivatives (3a-p) was synthesized with the aim of evaluating their antimycobacterial activity toward a strain of Mycobacterium tuberculosis H37Rv. Their chemical structures were confirmed by H-1-nuclear magnetic resonance (NMR) and electrospray mass spectrometry (ES-MS) spectral data, and elemental analysis. The in vitro antimycobacterial evaluation was performed according to the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) antituberculosis drug discovery program. Compound 3a, 4-fluorobenzoic acid [(2,6-dichlorophenyl) methylene]hydrazide, showed the highest inhibitory activity of all the compounds under study.Publication Metadata only Synthesis and characterization of novel hydrazide-hydrazones and the study of their structure-antituberculosis activity(ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2006) KAYMAKÇIOĞLU, BEDİA; Bedia, Kocyigit-Kaymakcioglu; Elcin, Oruc; Seda, Unsalan; Fatma, Kandemirli; Nathaly, Shvets; Sevim, Rollas; Dimoglo, AnatholyA series of hydrazide-hydrazones, based on a series of 4-substituted benzoic acid, were synthesized, and their structures were elucidated and screened for the antituberculosis activity against Mycobacterium tuberculosis H37Rv with the help of the BACTEC 460 radiometric system. Compound 3. 4-fluorobenzoic acid [((5-nitro)thiophen-2yl) methylene]hydrazide showed the highest inhibitory activity in this series. The search of pharmacophores was done by means of the Electronic-Topological Method (ETM). The model developed in this study is supposed to be applied to the design, preparation and screening of new compounds of similar structure in order to further test and optimize the model with the eventual goal of preparing new anti-tubercular agents. (c) 2006 Elsevier Masson SAS. All rights reserved.Publication Open Access Synthesis and Antimicrobial Activity of Some Novel Schiff Bases Containing 1,2,4-Triazole-3-thione(WWW PUBL PTE, 2010) KAYMAKÇIOĞLU, BEDİA; Calisir, M. M.; Kocyigit-Kaymakcioglu, B.; Ozbek, B.; Otuk, G.A series of Schiff bases (4a-j) were prepared by reacting 4-amino-5-(1-phenylethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione and substituted aromatic aldehydes. The chemical structures were confirmed by means of UV, (1)H NMR, IR, MS(API-ES) spectral data and elemental analysis. All the synthesized compounds were screened for their antimicrobial activity. Among the tested compounds, Schiff bases with 4-OH and 4-NO(2) substituent exhibited remarkable antimicrobial activity against all the tested microorganism.