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U¨mide Demir O¨ zkay,Leyla Yurttas¸,Yusuf O¨ zkay,Umut I˙ rfan U¨ c¸el,O¨ zgu¨r Devrim Can,Yusuf Ozturk 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.7
In this study, we synthesized eight novel1-phenyl-2-(4-substituted-piperazin-1-yl)-propanol derivativesand evaluated their antidepressant-like activities. Thechemical structures of the synthesised compounds wereelucidated by spectroscopy and elemental analyses. Potential antidepressant-like effects of the test compounds(20 mg kg-1) were investigated using the tail-suspensiontest and modified forced swimming test (MFST) in mice. Additionally, the spontaneous locomotor activity of themice was assessed using the activity cage apparatus. Boththe reference drug fluoxetine (20 mg kg-1) and the testcompounds 3a–3e and 3g significantly shortened theimmobility time of the mice in both the behavioural tests. These test compounds also increased the swimming time inMFST without any change in the climbing duration. Compounds 3c–3e and 3g were significantly more potent ininducing these effects than 3a and 3b. None of the compoundschanged the locomotor activities of the animals,thus antidepressant-like effects of test compounds werespecific. The findings support those of previous studies thatreported antidepressant-like activities of aryl alkanolpiperazine derivatives.
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Antimicrobial Activity of a New Series of Benzimidazole Derivatives
Yusuf Özkay,Yag˘ mur Tunall,Hülya Karaca,lIhan Is¸lkdag 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.9
Due to antimicrobial importance of benzimidazoles and hydrazones, some benzimidazolehydrazone compounds were synthesized to screen their antimicrobial activity. Structures of the synthesized compounds were elucidated by ^1H-NMR, IR and ES-MS spectral data and elemental analysis. The synthesized benzimidazole-hydrazones exhibited very weak antibacterial activity. However, antifungal activity of some of the synthesized compounds was very notable against Candida species. The compounds displaying important antifungal activity were screened for their toxicity. Artemia salina 96-well assay was used to determine cytotoxicity of the compounds. Tested compounds exhibited toxicity to different extents (LD_50 = 126.33-368.72 μg/mL). Nevertheless, determination of 3-14 folds higher LD_50 than minimum inhibitory concentration is a significant finding, which demonstrates that the compounds display antifungal activity at non-toxic concentration.
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Özgür Devrim Can,Ümide Demir Özkay,Zafer Aslm Kaplanclkll,Yusuf Öztürk 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.9
The aim of the present study was examining the effects of some 1,3,5-trisubstituted-2-pyrazoline derivatives on depression, anxiety and spontaneous locomotor activity parameters of mice. None of the compounds was effective at 50 mg/kg dose whereas at 100 and 200 mg/kg, pyrazoline-benzoxazole derivative test compound 4a and pyrazoline-benzimidazole derivative test compound 4d in the series were exhibited significant antidepressant effects in modified forced swimming tests. These two pyrazolines decreased the immobility and increased the swimming times of mice without any change in climbing durations suggesting the antidepressant- like effects of the test compounds. In spite of significant antidepressant effect, none of the compounds changed the exploratory parameters in hole-board tests or total numbers of spontaneous locomotor activities in activity cage measurements at any of the applied doses. In other words, neither anxiolytic nor sedative effects induced by the test compounds. The results obtained from this study supported the previous findings reporting the antidepressant activities of pyrazoline derivative compounds. Exact mechanism of the antidepressant action exhibited in the present study need to be clarified with further detailed investigations.
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Özgür Devrim Can,Mehlika Dilek Altlntop,Ümide Demir Özkay,Umut I · rfan Üçel,Bürge Dog˘ruer,Zafer Aslm Kaplanclkll 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.4
Novel thiadiazole derivatives bearing hydrazone moieties were synthesized through the reaction of 2-[(5-methyl-1,3,4-thiadiazol-2-yl)thio)]acetohydrazide with aldehydes/ketones. The chemical structures of the compounds were elucidated by 1H-NMR, 13C-NMR, MS-FAB spectral data, and elemental analyses. Behavioral effects of the test compounds in mice were examined by hole-board, activity cage, tail suspension and modified forced swimming tests (MFST). Antinociceptive activities were evaluated using the hot-plate and tail-clip methods. Results of the experiments indicated that the test compounds did not significantly change the exploratory behaviors or locomotor activities of animals in the hole-board and activity cage tests, respectively. Administration of the reference drug fluoxetine (10 mg/kg) and compounds 3a, 3b, 3c, 3j, 3k, and 3l significantly shortened the immobility times of animals in the tail suspension and MFST tests, indicating the antidepressant-like effects of these derivatives. Morphine (10 mg/kg) and compounds 3a, 3b, 3c, 3d, 3e, 3j, 3k, and 3l increased the reaction times of mice in both the hot-plate and tail-clip tests, indicating the antinociceptive effects of these compounds. To the best of our knowledge, this is the first study of central nervous system activities of chemical compounds carrying thiadiazole and hydrazone moieties together on their structures.
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