Person: KAYMAKÇIOĞLU, BEDİA
Loading...
Email Address
Birth Date
Research Projects
Organizational Units
Job Title
Last Name
KAYMAKÇIOĞLU
First Name
BEDİA
Name
31 results
Search Results
Now showing 1 - 10 of 31
Publication Metadata only Synthesis and biological activity of hydrazide-hydrazones and their corresponding 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles(SPRINGER BIRKHAUSER, 2012) KAYMAKÇIOĞLU, BEDİA; Kocyigit-Kaymakcioglu, Bedia; Oruc-Emre, Emine Elcin; Unsalan, Seda; Tabanca, Nurhayat; Khan, Shabana Iqrar; Wedge, David Earl; Iscan, Gokalp; Demirci, Fatih; Rollas, SevimVarious 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles (11-20) were prepared by the reaction of aryl substituted hydrazones of 4-fluorobenzoic acid hydrazide (1-10) with acetic anhydride. The structures of the synthesized compounds 11-20, were confirmed by UV, IR, H-1-NMR and mass spectroscopic methods. Antifungal evaluation of the hydrazide-hydrazones 1-10 and corresponding 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles 11-20, against clinical and standard Candida pathogens have been performed by using agar diffusion to indentify the active compounds, which were later subjected to a broth microdilution assay to justify the activity level in terms of minimum inhibitory concentrations (MIC). 4-Fluorobenzoic acid [(5-bromothiophen-2-yl)methylene]hydrazide, showed the highest inhibitory activity against Candida albicans (MIC: 125 mu g/ml), and when compared with ketoconazole. In addition, bioauthographic antifungal activity against plant pathogenic fungi such as Colletotrichum, Botrytis, Fusarium, and Phomopsis was conducted. 4-Fluorobenzoic acid [(5-bromothiophen-2-yl)methylene]hydrazide was the most active analog against P. viticola with 91% inhibition at 30 mu M after 144 h. Furthermore, known and the newly synthesized compounds were also screened through a panel of bioassays to determine their anti-inflammatory, cytotoxic, and antioxidant activities in mammalian cells. 3-Acetyl-5-(4-fluorophenyl)-2-(3-hydroxy-4-methoxyphenyl)-2,3-dihydro-1,3,4-oxadiazole, showed a strong inhibition of NF-kappa B-dependent transcription in SW1353 cells with IC50 value of 0.75 mu g/ml. 4-Fluorobenzoic acid [(3-hydroxy-4-methoxyphenyl)methylene]hydrazide, and 3-acetyl-5-(4-fluorophenyl)-2-(3-hydroxy-4-methoxyphenyl)-2,3-dihydro-1,3,4-oxadiazole on intracellular ROS generation in PMA induced HL-60 cells demonstrated potent activity with IC50 values of 0.9 mu g/ml. A strong inhibition of the activity of iNOS activity in LPS induced RAW 264.7 cells was observed for 3-acetyl-5-(4-fluorophenyl)-2-(4-hydroxyphenyl)-2,3-dihydro-1,3,4-oxadiazole with IC50 value of 0.3 mu g/ml.Publication Metadata only Studies on hydrazide-hydrazones derivatives as acetylcholinesterase inhibitors(AVES PRESS LTD, 2015) KAYMAKÇIOĞLU, BEDİA; Abu Mohsen, Usama; Kocyigit-Kaymakcioglu, Bedia; Oruc-Emre, Emine Elcin; Kaplancikli, Zafer Asim; Rollas, SevimObjective: Fifteen hidrazide-hydrazone derivatives were synthesized and evaluated for their ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman's spectrophotometric method. Methods: Anti-acetylcholinesterase activity was evaluated by using a modification of Ellman'sspectrophotometric method. The spectrophotometric method is based on the reaction of released thiocholine to give a coloured product with a chromogenic reagent 5,5-dithio-bis-(2-nitrobenzoic acid). Results: Among the tested compounds, 4-fluorobenzoic acid [(4-methoxyphenyl) methylene] hydrazide (6) and 2-[(fluorobenzoyl) hydrazono]-1,3-dihydro-indol-3-one (15), showed noteworthy anti-AChE activity when compared to standard drug donepezil (IC50=0.054 +/- 0.002 mu M). Conclusion: The anti-AChE activity screening indicated that among the tested compounds, 6 with p-methoxyphenyl substitution and 15 with1,3-dihydro- indol-3-one substitution represent the most active compounds. Based on the activity results, it appears that bulky groups on the hydrazide-hydrazone moiety have made good contribution to the anti-AChE activity.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 Bebeklerde pişik önleyici amaçla, biodegradable fiber kumaş içeren bitkisel içerikli ıslak mendillerin geliştirilmesi(2022-02-18) KAYMAKÇIOĞLU, BEDİA; ŞAHBAZ, SEVİNÇ; Akgil M., Aktı M., Şahbaz S., Kaymakçıoğlu B.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 of some novel azo derivatives of 3,5-dimethly-1-(2-hydroxyethyl)pyrazole as potent analgesic agents(WILEY-V C H VERLAG GMBH, 2006) KAYMAKÇIOĞLU, BEDİA; Oruc, E. E.; Kocyigit-Kaymakcioglu, B.; Oral, B.; Altunbas-Toklu, H. Z.; Kabasakal, L.; Rollas, S.A series of 1-(2-hydroxyethyl)-3,5-dimethylpyrazolylazo derivatives, incorporating thiosemicarbazide 2a-c, 1,3,4-thiadiazole 3a-c, and 1,2,4-triazole-3-thione 4a-c were synthesized. The structure of these novel synthesized compounds 2a-c, 3a-c, and 4a-c was confirmed by spectral analysis. All these compounds were screened for their analgesic activity. Hot-plate and tail-immersion tests were used for the determination of the analgesic activity. Morphine, an analgesic through both spinal and supraspinal pathways, was used as a standard test drug. All compounds were administered at a dose of 100 mg/kg i.p. Among the compounds, 2-(butylamino)-5-[((1-(2-hydroxyethyl)-3,5-dimethylpyrazole-4-yl)azo)phenyl]-1,3,4-thiadiazole 3a and 4-[((1-(2-hydroxyethyl)-3,5dimethylpyrazole-4-yl)azo)phenyl]-4-(2-phenethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 4c showed analgesic effects in both tests. Especially 4c exerted strong analgesia starting at 30 min after injection.Publication Metadata only Pirazolon halkası taşıyan bazı Schiff bazlarının biyolojik etkilerinin incelenmesi(2018-11-16) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; UĞRAŞ Z., TOK F., KAYMAKÇIOĞLU B.Publication Metadata only Synthesis, anticancer evaluation and in silico ADMET studies on urea/thiourea derivatives from gabapentin(TAYLOR & FRANCIS LTD, 2020) KAYMAKÇIOĞLU, BEDİA; Turk, Sevda; Tok, Fatih; Erdogan, Omer; Cevik, Ozge; Tok, Tugba Taskin; Kocyigit-Kaymakcioglu, Bedia; Karakus, Sevgi2-(1-((3-Substitutedureido/thioureido)methyl)cyclohexyl)acetic acid derivatives (1-9) were synthesized from gabapentin. All the synthesized compounds were characterized by using IR, H-1-NMR, C-13-NMR spectroscopy, mass spectrometry and elemental analysis. Urea and thiourea derivatives were investigated for their potential in vitro anticancer activities on PC3 and MCF7 cancer cell lines using MTT assay. Cell apoptosis was detected by with Annexin V Assay. Our results showed that compound 8 {2-(1-((3-(2,6-dichlorophenyl)ureido)methyl)cyclohexyl)acetic acid} significantly inhibited the proliferation and growing of PC3 and MCF7 cells. Both cell types showed dysfunction of cellular morphology which induced apoptosis 10 mu M concentration of compound 8 treated cells. Our results indicate that compound 8 might have significance as an anti-tumor agent against human prostate and breast cancer. The theoretical structure and activity estimation via in silico ADMET was also examined.Publication Metadata only Pirazolon halkasından hareketle sentezlenen çeşitli Schiff bazları üzerinde saflaştırmaçalışmaları(2018-11-16) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; Yılmaz S., TOK F., KAYMAKÇIOĞLU B.