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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), (1)H Nuclear Magnetic Resonance Spectroscopy ((1)H-NMR), (13)C Nuclear Magnetic Reso...

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Autores principales: Can, Nafiz Öncü, Can, Özgür Devrim, Osmaniye, Derya, Demir Özkay, Ümide
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017710/
https://www.ncbi.nlm.nih.gov/pubmed/29561803
http://dx.doi.org/10.3390/molecules23040716
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author Can, Nafiz Öncü
Can, Özgür Devrim
Osmaniye, Derya
Demir Özkay, Ümide
author_facet Can, Nafiz Öncü
Can, Özgür Devrim
Osmaniye, Derya
Demir Özkay, Ümide
author_sort Can, Nafiz Öncü
collection PubMed
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), (1)H Nuclear Magnetic Resonance Spectroscopy ((1)H-NMR), (13)C Nuclear Magnetic Resonance Spectroscopy ((13)C-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.
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spelling pubmed-60177102018-11-13 Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities Can, Nafiz Öncü Can, Özgür Devrim Osmaniye, Derya Demir Özkay, Ümide Molecules Article 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), (1)H Nuclear Magnetic Resonance Spectroscopy ((1)H-NMR), (13)C Nuclear Magnetic Resonance Spectroscopy ((13)C-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. MDPI 2018-03-15 /pmc/articles/PMC6017710/ /pubmed/29561803 http://dx.doi.org/10.3390/molecules23040716 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Can, Nafiz Öncü
Can, Özgür Devrim
Osmaniye, Derya
Demir Özkay, Ümide
Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities
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 Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017710/
https://www.ncbi.nlm.nih.gov/pubmed/29561803
http://dx.doi.org/10.3390/molecules23040716
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