Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities
Novel thiadiazole derivatives were synthesized through the reaction of acetylated 2-aminothiadiazole and piperazine derivatives. The chemical structures of the compounds were clarified by Infrared Spectroscopy (IR), 1H Nuclear Magnetic Resonance Spectroscopy (1H-NMR), 13C Nuclear Magnetic Resonance...
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MDPI AG
2018-03-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/23/4/716 |
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| author | Nafiz Öncü Can Özgür Devrim Can Derya Osmaniye Ümide Demir Özkay |
| author_facet | Nafiz Öncü Can Özgür Devrim Can Derya Osmaniye Ümide Demir Özkay |
| author_sort | Nafiz Öncü Can |
| collection | DOAJ |
| description | Novel thiadiazole derivatives were synthesized through the reaction of acetylated 2-aminothiadiazole and piperazine derivatives. The chemical structures of the compounds were clarified by Infrared Spectroscopy (IR), 1H Nuclear Magnetic Resonance Spectroscopy (1H-NMR), 13C Nuclear Magnetic Resonance Spectroscopy (13C-NMR) and Electronspray Ionisation Mass Spectroscopy (ESI-MS) spectroscopic methods. Antidepressant-like activities were evaluated by the tail-suspension (TST) and modified forced swimming (MFST) methods. Besides, possible influence of the test compounds on motor activities of the animals were examined by activity cage tests. In the TST, administration of the compounds 2c, 2d, 2e, 2f, 2g and 2h significantly decreased the immobility time of mice regarding the control values. Further, in the MFST, the same compounds reduced the total number of immobility behaviors while increasing swimming performance. However, no change was observed in the total number of climbing behaviors. These data suggested that compounds 2c, 2d, 2e, 2f, 2g and 2h possess notable antidepressant-like activities. Reference drug fluoxetine (10 mg/kg) was also exhibited its antidepressant activity, as expected. No significant difference was seen between the locomotor activity values of the test groups signifying that observed antidepressant-like activities are specific. Theoretical calculation of absorption, distribution, metabolism, excretion (ADME) properties for the obtained compounds were performed and obtained data supported the antidepressant-like potential of these novel thiadiazole derivatives. |
| first_indexed | 2024-04-13T12:10:33Z |
| format | Article |
| id | doaj.art-5794aea40b14490c9d3167029032183b |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-04-13T12:10:33Z |
| publishDate | 2018-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-5794aea40b14490c9d3167029032183b2022-12-22T02:47:29ZengMDPI AGMolecules1420-30492018-03-0123471610.3390/molecules23040716molecules23040716Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like ActivitiesNafiz Öncü Can0Özgür Devrim Can1Derya Osmaniye2Ümide Demir Özkay3Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, TurkeyDepartment of Pharmacology, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, TurkeyDoping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, TurkeyDepartment of Pharmacology, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, TurkeyNovel thiadiazole derivatives were synthesized through the reaction of acetylated 2-aminothiadiazole and piperazine derivatives. The chemical structures of the compounds were clarified by Infrared Spectroscopy (IR), 1H Nuclear Magnetic Resonance Spectroscopy (1H-NMR), 13C Nuclear Magnetic Resonance Spectroscopy (13C-NMR) and Electronspray Ionisation Mass Spectroscopy (ESI-MS) spectroscopic methods. Antidepressant-like activities were evaluated by the tail-suspension (TST) and modified forced swimming (MFST) methods. Besides, possible influence of the test compounds on motor activities of the animals were examined by activity cage tests. In the TST, administration of the compounds 2c, 2d, 2e, 2f, 2g and 2h significantly decreased the immobility time of mice regarding the control values. Further, in the MFST, the same compounds reduced the total number of immobility behaviors while increasing swimming performance. However, no change was observed in the total number of climbing behaviors. These data suggested that compounds 2c, 2d, 2e, 2f, 2g and 2h possess notable antidepressant-like activities. Reference drug fluoxetine (10 mg/kg) was also exhibited its antidepressant activity, as expected. No significant difference was seen between the locomotor activity values of the test groups signifying that observed antidepressant-like activities are specific. Theoretical calculation of absorption, distribution, metabolism, excretion (ADME) properties for the obtained compounds were performed and obtained data supported the antidepressant-like potential of these novel thiadiazole derivatives.http://www.mdpi.com/1420-3049/23/4/716activity cagemodified forced swimmingtail-suspensionthiadiazole |
| spellingShingle | Nafiz Öncü Can Özgür Devrim Can Derya Osmaniye Ümide Demir Özkay Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities Molecules activity cage modified forced swimming tail-suspension thiadiazole |
| title | Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities |
| title_full | Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities |
| title_fullStr | Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities |
| title_full_unstemmed | Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities |
| title_short | Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities |
| title_sort | synthesis of some novel thiadiazole derivative compounds and screening their antidepressant like activities |
| topic | activity cage modified forced swimming tail-suspension thiadiazole |
| url | http://www.mdpi.com/1420-3049/23/4/716 |
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