Person: KAYMAKÇIOĞLU, BEDİA
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KAYMAKÇIOĞLU
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BEDİA
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Publication Open Access Synthesis and anticancer activity of new carbohydrazide derivatives bearing furan moiety(MARMARA UNIV, 2022) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Kaya Tilki, Elif; Dikmen, Miris; Kocyigit-Kaymakcioglu, BediaPublication 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 Metadata only Novel 2,5-disubstituted-1,3,4-oxadiazole derivatives as MAO-B inhibitors: Synthesis, biological evaluation and molecular modeling studies(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2021) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Ugras, Zefine; Saglik, Begum Nurpelin; Ozkay, Yusuf; Kaplancikli, Zafer Asim; Kocyigit-Kaymakcioglu, BediaThirty novel 2,5-disubstituted-1,3,4-oxadiazole derivatives bearing urea moiety were designed and synthesized. IR, 1H-NMR, 13C-NMR and mass spectroscopic methods and elemental analysis were used to confirm the structures of the compounds. Their monoamine oxidase inhibitory activity was determined against the MAO-A and MAO-B isoforms. None of the compounds showed the potent MAO-A inhibitory activity, while the MAO-B inhibition was significantly found in the range of 62 to 98%. Among them, the compounds H8, H9 and H12 bearing chloro substituent at the fourth position of phenylurea were found to show potent monoamine oxidase B inhibitory activity with IC50 values 0.039-0.066 mu M. To define and evaluate the interaction mechanism between compound H8 and monoamine oxidase B, molecular docking studies have been made.Publication Metadata only Synthesis of new hydrazone derivatives and evaluation of their monoamine oxidase inhibitory activity(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2021) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Saglik, Begum Nurpelin; Ozkay, Yusuf; Ilgin, Sinem; Kaplancikli, Zafer Asim; Kocyigit-Kaymakcioglu, BediaA novel series of hydrazone derivatives were designed and synthesized. Their structures were characterized by IR, 1H NMR, 13C NMR and HR-MS spectroscopic methods. The newly synthesized compounds were evaluated for their inhibitory activity against monoamine oxidase enzymes (MAO-A and MAO-B). Compounds 2a, 2k, 4a and 4i showed significant inhibitory activity against MAO-A, with IC50 value in the range of 0.084-0.207 mu M compared to reference drug moclobemide (IC50 value = 6.061 mu M). These compounds (2a, 2k, 4a and 4i) were exposed to cytotoxicity tests to establish their preliminary toxicological profiles and were found to be noncytotoxic. Moreover, the most effective compound 4i was evaluated using enzyme kinetics and docking studies to elucidate the plausible mechanisms of inhibition of MAO-A. According to enzyme kinetic studies, compound 4i was a reversible and competitive inhibitor with similar inhibition features as the substrates. Also, it was seen that this compound was settled down very properly at the active site of MAO-A enzyme by doing important interactions owing to the docking studies. Finally, ADME predictions were applied to estimate pharmacokinetic profiles of synthesized compounds. According to calculated ADME predictions, all parameters of the compounds were within the standard ranges in terms of Rule of Five and Rule of Three and it was detected that the synthesized compounds (2a-4i) have good and promising pharmacokinetic profiles.Publication Open Access Synthesis and antinociceptive-antimicrobial activities of some new amide derivatives of 3,5-di/-and 1,3,5-trimethylpyrazoles(TAYLOR & FRANCIS LTD, 2008-01-01) KAYMAKÇIOĞLU, BEDİA; Kocyigit-Kaymakcioglu, Bedia; Toklu, Hale Z.; Ikiz, Serkan; Bagcigil, A. Funda; Rollas, Sevim; Ozgur, N. Yakut; Ak, SeyyalSome N-(3,5-di-/1,3,5-trimethylpyrazole-4-yl)-4-substitutedbenzamide derivatives were prepared as possible antiociceptive-antimicrobial agents. New amide derivatives (3-12) were synthesized by reacting 4-amino-3,5-di and 1,3,5-trimethylpyrazoles with 4-substitutedbenzoyl chlorides. Hotplate and tail-immersion tests were used for the determination of the antinociceptive activity. Morphine, was used as a standard test drug. All compounds were administered at a dose of 100 mg/kg ip and some of them had significant antinociceptive activity in both tests. Compound 10 (N-(1,3,5-trimethylpyrazole-4-yl)-4-bromobenzamide), was the most active one in both tests among the compounds. The antinociceptive activity of the compounds 10, 11 (N-(1,3,5-trimethylpyrazole-4-yl)-4-chlorobenzamide), and 12 (N-(1,3,5-trimethylpyrazole-4-yl)-4-fluorobenzamide), started at 30 minutes and continued up to 150 minutes in the hotplate test. Also compounds were tested for their in vitro antimicrobial activity, but exhibited weak antibacterial activity.Publication Open Access Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties(MDPI, 2013-03-19) KAYMAKÇIOĞLU, BEDİA; Kocyigit-Kaymakcioglu, Bedia; Celen, Ahmet Ozgur; Tabanca, Nurhayat; Ali, Abbas; Khan, Shabana I.; Khan, Ikhlas A.; Wedge, David E.A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity. Triazole derivatives 3a-e and 4a-e were synthesized by reacting thiocarbohydrazide with thiourea and urea compounds 1a-e and 2a-e, respectively, in a 130-140 degrees C oil bath. The proposed structures of all the synthesized compounds were confirmed using elemental analysis, UV, IR, H-1-NMR and mass spectroscopy. All compounds were evaluated for antifungal activity against plant pathogens, larvicidal and biting deterrent activity against the mosquito Aedes aegypti L. and in vitro cytotoxicity and anti-inflammatory activity against some human cell lines. Phomopis species were the most sensitive fungi to these compounds. Compounds 1b, 1c, 3a and 4e demonstrated selectively good activity against Phomopis obscurans and only 1b and 4e showed a similar level of activity against P. viticola. Compound 3d, with a LD50 value of 67.9 ppm, followed by 1c (LD50 = 118.8 ppm) and 3e (LD50 = 165.6 ppm), showed the highest toxicity against Aedes aegypti larvae. Four of these compounds showed biting deterrent activity greater than solvent control, with the highest activity being seen for 1c, with a proportion not biting (PNB) value of 0.75, followed by 1e, 2b and 1a. No cytotoxicity was observed against the tested human cancer cell lines. No anti-inflammatory activity was observed against NF-kappa B dependent transcription induced by phorbol myristate acetate (PMA) in human chondrosarcoma cells.Publication Metadata only Synthesis and Anticonvulsant Activity of New N-(Alkyl/Substituted aryl)-N '-[4-(5-cyclohexylamino)-1,3,4-thiadiazole-2-yl)pheny]thioureas(WILEY-V C H VERLAG GMBH, 2009) KAYMAKÇIOĞLU, BEDİA; Karakus, Sevgi; Kocyigit-Kaymakcioglu, Bedia; Toklu, Hale Z.; Aricioglu, Feyza; Rollas, SevimA series of novel thiourea derivatives carrying the 5-cylohexylamino-1,3,4-thiadiazole moiety was synthesized and their anticonvulsant activity was evaluated. Structures of the synthesized compounds have been confirmed by IR, H-1-NMR, and elemental analysis. All of the compounds were administered at a dose of 50 mg/kg. Some of the active compounds have different effects in pentylenetetrazole (PTZ) and maximal electroshock (MES) tests, indicating the therapeutical potential in petit mal seizures, but not in grand mal seizures. Compounds 10, 11, 13, and 14 carrying 2-methylphenyl, 4-chlorophenyl, allyl, and 4-methylphenyl on the thiourea pharmacophore, increased the survival rate in the PTZ model. The ED50 values of the active compounds 10, 11, 13, and 14 were found 68.42, 43.75, 18.75 and 25 mg/kg, respectively.Publication Metadata only SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NEW HYDRAZONE DERIVATIVES BEARING PYRIMIDINE RING AS ANALGESIC AND ANTI-INFLAMMATORY AGENTS(POLSKIE TOWARZYSTWO FARMACEUTYCZNE, 2018) KAYMAKÇIOĞLU, BEDİA; Akdag, Kadryiye; Unal, Gokhan; Tok, Fatih; Aricioglu, Feyza; Temel, Halide Edip; Kocyigit-Kaymakcioglu, BediaNew hydrazone derivatives were synthesized from 4-chloro-2-(methylthio) pyrimidine-5-carbohydrazide. IR, 1H-NMR, 13C-NMR, mass spectral data and elemental analysis characterized synthesized compounds. All compounds were investigated for analgesic and anti-inflammatory activity with hot plate test and biochemical assay, respectively. The results of anti-inflammatory activity showed that compound 2t had maximal lipoxygenase (LOX) inhibition (66.30%) whereas inhibitions of 2a, 2c, 2i, 2k, 2l, 2m, 2p, 2s, and 2u were observed between approximately 45-15%. Our results also indicated that 15 compounds of 21 had an analgesic effect in hot plate test. Analgesic effect of 2l, 2s, 2t began earlier than others while the effect of 2i began at the latest time. According to the activity results, compound 2t have both significant analgesic and anti-inflammatory effects.Publication Open Access Synthesis and structure-activity relationships of carbohydrazides and 1,3,4-oxadiazole derivatives bearing an imidazolidine moiety against the yellow fever and dengue vector, Aedes aegypti(JOHN WILEY & SONS LTD, 2018-02) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Kocyigit-Kaymakcioglu, Bedia; Tabanca, Nurhayat; Estep, Alden S.; Gross, Aaron D.; Geldenhuys, Werner J.; Becnel, James J.; Bloomquist, Jeffrey R.BACKGROUND 1,3,4-Oxadiazole and imidazolidine rings are important heterocyclic compounds exhibiting a variety of biological activities. In this study, novel compounds with oxadiazole and imidazolidine rings were synthesized from 3-(methylsulfonyl)-2-oxoimidazolidine-1-carbonyl chloride and screened for insecticidal activities. The proposed structures of the 17 synthesized compounds were confirmed using elemental analysis, infrared (IR), proton nuclear magnetic resonance (H-1-NMR), and mass spectroscopy. RESULTS None of the compounds showed larvicidal activity at the tested concentrations against first-instar Aedes aegypti larvae. However, nine compounds exhibited promising adulticidal activity, with mortality rates of >= 80% at 5 mu g per mosquito. Further dose-response bioassays were undertaken to determine median lethal dose (LD50) values. Compounds 1, 2b, 2c, 2d, 2 g, 3b, 3c, 3 g, and 3 h were effective, with typical LD50 values of about 5 - 10 mu g per mosquito against female Ae. aegypti. Compounds 2c (bearing a nitro group on the aromatic ring; LD50 = 2.80 0.54 mu g per mosquito) and 3 h (double halogen groups at 2,4 position on the phenyl ring; LD50 = 2.80 +/- 0.54 mu g per mosquito) were the most promising compounds. CONCLUSION Preliminary mode of action studies failed to show consistent evidence of either neurotoxic or mitochondria-directed effects. Further chemical synthesis within this series may lead to the development of new effective insecticides. (C) 2017 Society of Chemical IndustryPublication 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.