Studies on the Anticonvulsant Activity and Influence on  GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione- Based Compounds

Plech, Tomasz; Kaproń, Barbara; Łuszczki, Jarogniew J.; Wujec, Monika; Paneth, Agata; Siwek, Agata; Kołaczkowski, Marcin; Żołnierek, M.; Nowak, Gabriel

doi:10.3390/molecules190811279

Cited by 45 publications

(40 citation statements)

References 34 publications

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“…The following 1,2,4-triazole-3-thione derivatives were investigated during current studies: 5-(3-chlorophenyl)-4-(4-methylphenyl)-2,4dihydro-3H-1,2,4-triazole-3-thione (TP-10), 5-(3-chlorophenyl)-4hexyl-2,4-dihydro-3H-1,2,4-triazole-3-thione (TP-315), and 5-(3chlorobenzyl)-4-hexyl-2,4-dihydro-3H-1,2,4-triazole-3-thione (TP-427). The compounds were synthesised according to procedures described in our previously published papers [13][14][15] .…”

Section: Investigated Drugsmentioning

confidence: 99%

“…Inhibitory activity of TP-10, TP-315, and TP-427 against human carbonic anhydrase isoforms I and II (hCA I, hCA II) was determined using a stopped flow technique. Acetazolamide (AAZ), being a clinically used CA inhibitor, was used as a reference drug ( Data for levetiracetam and valproate are taken from Barton et al 25 Median toxic doses (TD50) are taken from our previous papers [13][14][15] . concentrations (i.e.…”

Section: Effect Of Tp-10 Tp-315 Tp-427 On the Activity Of Human Carmentioning

confidence: 99%

“…MES test) and favourable ADME-Tox properties (long-lasting effect, low toxicity, lack of genotoxic properties, etc.) [10][11][12][13][14][15][16] . These compounds exhibited fast onset of action and some of them were able to potentiate the anticonvulsant activity of valproate, which is the most commonly prescribed antiepileptic drug.…”

Section: Introductionmentioning

confidence: 99%

“…Chemical structure and pharmacological properties of the most active 1,2,4-triazole-3-thione derivatives11,[13][14][15] .…”

mentioning

confidence: 99%

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1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy

Kaproń

Czarnomysy

Wysokiński

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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There are numerous studies supporting the contribution of oxidative stress to the pathogenesis of epilepsy. Prolonged oxidative stress is associated with the overexpression of ATP-binding cassette transporters, which results in antiepileptic drugs resistance. During our studies, three 1,2,4-triazole-3-thione derivatives were evaluated for the antioxidant activity and anticonvulsant effect in the 6 Hz model of pharmacoresistant epilepsy. The investigated compounds exhibited 2-3 times more potent anticonvulsant activity than valproic acid in 6 Hz test in mice, which is well-established preclinical model of pharmacoresistant epilepsy. The antioxidant/ROS scavenging activity was confirmed in both single-electron transferbased methods (DPPH and CUPRAC) and during flow cytometric analysis of total ROS activity in U-87 MG cells. Based on the enzymatic studies on human carbonic anhydrases (CAs), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), one can assume that the herein investigated drug candidates will not impair the cognitive processes mediated by CAs and will have minimal off-target cholinergic effects. ARTICLE HISTORY

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Section: Investigated Drugsmentioning

confidence: 99%

Section: Effect Of Tp-10 Tp-315 Tp-427 On the Activity Of Human Carmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

“…Chemical structure and pharmacological properties of the most active 1,2,4-triazole-3-thione derivatives11,[13][14][15] .…”

mentioning

confidence: 99%

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1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy

Kaproń

Czarnomysy

Wysokiński

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Characteristic features of all active compounds were a rapid onset of action and long lasting effects. Compound 126 exhibited the most potent activity (ED 50 = 35.2 mg/kg) ( Table 6) [107].…”

Section: The Indoline-2 3-dione Functional Groupmentioning

confidence: 99%

Current Research on Antiepileptic Compounds

2015

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Epilepsy affects about 1% of the world's population. Due to the fact all antiepileptic drugs (AEDs) have some undesirable side effects and about 30% of epileptic patients are not seizure-free with the existing AEDs, there is still an urgent need for the development of more effective and safer AEDs. Based on our research work on antiepileptic compounds and other references in recent years, this review covers the reported work on antiepileptic compounds which are classified according to their structures. This review summarized 244 significant anticonvulsant compounds which are classified by functional groups according to the animal model data, although there are some limitations in the data. This review highlights the properties of new compounds endowed with promising antiepileptic properties, which may be proven to be more effective and selective, and possibly free of unwanted side effects. The reviewed compounds represent an interesting possibility to overcome refractory seizures and to reduce the percentage of patients with a poor response to drug therapy.

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Synthesis and Antibacterial Evaluation of Mannich Bases Derived from 1,2,4‐Triazole

Paneth

Trotsko

Popiołek

et al. 2019

Chemistry & Biodiversity

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The series of novel Mannich bases were synthesized and evaluated for their in vitro antibacterial activity against Gram‐positive and Gram‐negative bacterial strains. The results showed that all compounds were less active than the drugs used as reference, but some of them had moderate potency against Staphylococcus epidermidis ATCC 12228 and Bacillus subtilis ATCC 6633. The presence of a phenyl ring in the position 4 of piperazine seems to be necessary for antibacterial activity in this class of compounds.

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Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione- Based Compounds

Cited by 45 publications

References 34 publications

1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy

1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy

Current Research on Antiepileptic Compounds

Synthesis and Antibacterial Evaluation of Mannich Bases Derived from 1,2,4‐Triazole

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