A5077746708- Neuroscience and Neuropharmacology Research
- Chemical Reaction Mechanisms
- Coordination Chemistry and Organometallics
- Synthesis of heterocyclic compounds
- Epilepsy research and treatment
- Phenothiazines and Benzothiazines Synthesis and Activities
- Pharmacological Effects and Toxicity Studies
- Pharmacological Receptor Mechanisms and Effects
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Chemical Synthesis and Analysis
- Cholinesterase and Neurodegenerative Diseases
- Ion channel regulation and function
- Synthesis and pharmacology of benzodiazepine derivatives
- Asymmetric Synthesis and Catalysis
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Inorganic and Organometallic Chemistry
- Fluorine in Organic Chemistry
- Synthesis and Biological Evaluation
- Pregnancy and preeclampsia studies
- Pain Mechanisms and Treatments
- Synthesis and biological activity
- Analytical Chemistry and Chromatography
- Synthesis and Reactions of Organic Compounds
- Alcoholism and Thiamine Deficiency
Jagiellonian University
2016-2025
Medicina
2015-2024
Medical University of Lublin
1995-2016
Państwowa Wyższa Szkoła Zawodowa w Nysie
2011
University of Economics and Innovation
2003
Górnośląskie Centrum Medyczne
2000
The library of 27 new 1-(4-phenylpiperazin-1-yl)- or 1-(morpholin-4-yl)-(2,5-dioxopyrrolidin-1-yl)propanamides and (2,5-dioxopyrrolidin-1-yl)butanamides as potential hybrid anticonvulsant agents was synthesized. These molecules join the chemical fragments well-known antiepileptic drugs (AEDs) such ethosuximide, levetiracetam, lacosamide. Compounds 5, 10, 11, 24 displayed broad spectra activity across preclinical seizure models, namely, maximal electroshock (MES) test, subcutaneous...
Studies have revealed that inhibition of glycine transporter type 1 (GlyT1) may provide a balanced regulation between excitation and in some brain structures and, thereby, modulate seizure activity. Data on the role GlyT1 epilepsy are, however, very limited. Here, we examined effect SSR504734, highly selective reversible inhibitor, three acute tests mice. We also evaluated its impact neurotransmitter levels relevant following seizures, possible adverse effects, changes inflammatory mediators...
Recently, compound KA-11 was identified as a promising candidate for new broad-spectrum anticonvulsant. This revealed wide protective activity across the most important animal models of seizures such maximal electroshock test (MES), subcutaneous pentylenetetrazole (scPTZ), and six-hertz (6 Hz, 32 mA). Importantly, devoid acute neurological activity, which assessed by applying chimney (TD50 value higher than 1500 mg/kg). The preliminary in vivo results confirmed favorable anticonvulsant...
The focused set of new pyrrolidine-2,5-diones as potential broad-spectrum hybrid anticonvulsants was described. These derivatives integrate on the common structural scaffold chemical fragments well-known antiepileptic drugs such ethosuximide, levetiracetam, and lacosamide. Such hybrids demonstrated effectiveness in two most widely used animal seizure models, namely, maximal electroshock (MES) test psychomotor 6 Hz (32 mA) models. Compound 33 showed highest anticonvulsant activity these...
We developed a focused set of original hybrid pyrrolidine-2,5-dione derivatives with potent anticonvulsant and antinociceptive properties. These compounds demonstrated broad-spectrum protective activity in range mouse models, such as the maximal electroshock (MES) test, pentylenetetrazole-induced seizures (scPTZ), 6 Hz (32 mA) seizures. Compound 22 showed most (ED50 MES = 23.7 mg/kg, ED50 22.4 ED50scPTZ 59.4 mg/kg). In addition, revealed efficacy formalin-induced tonic pain. vivo activities...
(R)-7 [(R)-AS-1] showed broad-spectrum antiseizure activity across in vivo mouse seizure models: maximal electroshock (MES), 6 Hz (32/44 mA), acute pentylenetetrazol (PTZ), and PTZ-kindling. A remarkable separation between CNS-related adverse effects was also observed. In vitro studies with primary glia cultures COS-7 cells expressing the glutamate transporter EAAT2 enhancement of uptake, revealing a stereoselective positive allosteric modulator (PAM) effect, further supported by molecular...
In our recent studies, we identified compound N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide (AS-1) as a broad-spectrum hybrid anticonvulsant which showed potent protection across the most important animal acute seizure models such maximal electroshock (MES) test, subcutaneous pentylenetetrazole (s.c. PTZ) and 6-Hz (32 mA) test in mice. Therefore, AS-1 may be recognized candidate for new effective different types of human epilepsy with favorable safety margin profile determined rotarod aim...
Abstract A series of new Mannich bases N ‐[(4‐arylpiperazin‐1‐yl)‐methyl]‐3‐(chlorophenyl)‐pyrrolidine‐2,5‐diones 10–23 have been synthesized and evaluated for their anticonvulsant activity in maximum electroshock (MES) subcutaneous pentylenetetrazole ( sc PTZ) seizure threshold tests. Their neurotoxicity was determined using a rotorod screen. Several molecules showed promising profile especially the MES‐test. In this model seizures, most active were...