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Molecules 2018, 23(4), 716; https://doi.org/10.3390/molecules23040716

Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities

1
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey
2
Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey
3
Department of Pharmacology, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey
4
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey
*
Author to whom correspondence should be addressed.
Received: 7 February 2018 / Revised: 1 March 2018 / Accepted: 7 March 2018 / Published: 21 March 2018
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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. View Full-Text
Keywords: activity cage; modified forced swimming; tail-suspension; thiadiazole activity cage; modified forced swimming; tail-suspension; thiadiazole
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Can, N.Ö.; Can, Ö.D.; Osmaniye, D.; Demir Özkay, Ü. Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities. Molecules 2018, 23, 716.

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