Person: KAYMAKÇIOĞLU, BEDİA
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KAYMAKÇIOĞLU
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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 Open Access Synthesis and anticonvulsant activity of substituted thiourea derivatives(2011-01-01) KAYMAKÇIOĞLU, BEDİAPublication 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 Metadata only Synthesis and biological evaluation of new N-substituted-N '-(3,5-di/1,3,5-trimethylpyrazole-4-yl)thiourea/urea derivatives(ELSEVIER SCIENCE BV, 2005) KAYMAKÇIOĞLU, BEDİA; Kaymakcioglu, BK; Rollas, S; Korcegez, E; Aricioglu, FSeveral thiourea and urea derivatives were prepared by the reaction of 4-aminopyrazoles with substituted isothiocyanates or isocyanates. The novel compounds were tested anticonvulsant activity using by pentylenetetrazole-induced seizure (PTZ) and maximal electroshock seizure (MES) tests. Among the tested compounds, thiourea derivatives of 4b were afforded 90 and 100% protection in PTZ and MES tests at 50 mg/kg, respectively. Urea derivatives of 5a and 5b were afforded 82 and 100% protection both at 25 and 50 mg/kg. Also synthesized compounds were screened for antituberculosis activity against Mycobacterium tuberculosis H(37)Rv at 6.25 mu g/mL concentration but they were not found active at these concentration. In addition, some selected compounds were evaluated for in vitro anti-HIV activity and they were all negative. (c) 2005 Elsevier B.V. All rights reserved.