Search results for: Karolina Słoczyńska

Items from 1 to 15 out of 15 results

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Biotransformation of 4‐fluoro‐N‐(1‐{2‐[(propan‐2‐yl)phenoxy]ethyl}‐8‐azabicyclo[3.2.1]octan‐3‐yl)‐benzenesulfonamide, a novel potent 5‐HT₇ receptor antagonist with antidepressant‐like and anxiolytic properties: In vitro and in silico approach

Karolina Słoczyńska, Katarzyna Wójcik‐Pszczoła, Vittorio Canale, Paweł Żmudzki, more

Journal of Biochemical and Molecular Toxicology > 32 > 5 > n/a - n/a

The aim of the study was to investigate the metabolism of 4‐fluoro‐N‐(1‐{2‐[(propan‐2‐yl)phenoxy]ethyl}‐8‐azabicyclo[3.2.1]octan‐3‐yl)‐benzenesulfonamide (PZ‐1150), a novel 5‐HT₇ receptor antagonist with antidepressant‐like and anxiolytic properties, by the following three ways: in vitro with microsomes; in vitro employing Cunninghamella echinulata, and in silico using MetaSite. Biotransformation...

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In Vitro Biotransformation, Safety, and Chemopreventive Action of Novel 8-Methoxy-Purine-2,6-Dione Derivatives

Małgorzata Anna Marć, Enrique Domínguez-Álvarez, Karolina Słoczyńska, Paweł Żmudzki, more

Applied Biochemistry and Biotechnology > 2018 > 184 > 1 > 124-139

Metabolic stability, mutagenicity, antimutagenicity, and the ability to scavenge free radicals of four novel 8-methoxy-purine-2,6-dione derivatives (compounds 1–4) demonstrating analgesic and anti-inflammatory properties were determined. Metabolic stability was evaluated in Cunninghamella and microsomal models, mutagenic and antimutagenic properties were assessed using the Ames and the Vibrio harveyi...

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Design, synthesis, and anticonvulsant activity of some derivatives of xanthone with aminoalkanol moieties

Anna M. Waszkielewicz, Karolina Słoczyńska, Elżbieta Pękala, Paweł Żmudzki, more

Chemical Biology & Drug Design > 89 > 3 > 339 - 352

A series of new xanthone derivatives have been synthesized and evaluated for their anticonvulsant properties in the maximal electroshock, subcutaneous metrazole tests and for neurotoxicity in the rotarod in mice, i.p. and rats, p.o. Compound 9: R,S‐2‐{2‐[(1‐hydroxybutan‐2‐yl]amino)ethoxy}‐9H‐xanthen‐9‐one and compound 12: R,S‐2‐{3‐[(1‐hydroxybutan‐2‐yl)amino]propoxy}‐9H‐xanthen‐9‐one exerted activity...

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Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH3 or 2-CH3

Agnieszka Gunia-Krzyżak, Dorota Żelaszczyk, Anna Rapacz, Ewa Żesławska, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 2 > 471-482

A series of twenty two (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH₃ or 2-CH₃ was designed, synthesized and evaluated for anticonvulsant activity in rodent models of seizures: maximal electroshock (MES) test, subcutaneous pentylenetetrazole (scPTZ) test, and 6-Hz test. There were identified three most active compounds: S-(2E)-N-(1-hydroxypropan-2-yl)-3-(2-methylphenyl)prop-2-enamide...

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In vitro mutagenic, antimutagenic, and antioxidant activities evaluation and biotransformation of some bioactive 4‐substituted 1‐(2‐methoxyphenyl)piperazine derivatives

Karolina Słoczyńska, Katarzyna Pańczyk, Anna M. Waszkielewicz, Henryk Marona, more

Journal of Biochemical and Molecular Toxicology > 30 > 12 > 593 - 601

In vitro mutagenic, antimutagenic, and antioxidant potency evaluation and biotransformation of six novel 4‐substituted 1‐(2‐methoxyphenyl)piperazine derivatives demonstrating antidepressant‐like activity were investigated. Mutagenic and antimutagenic properties were assessed using the Ames test; free radical scavenging activity was evaluated with 2,2‐diphenyl‐1‐picrylhydrazyl radical scavenging assay...

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N-Alkylated arylsulfonamides of (aryloxy)ethyl piperidines: 5-HT7 receptor selectivity versus multireceptor profile

Vittorio Canale, Rafał Kurczab, Anna Partyka, Grzegorz Satała, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 2 > 130-139

The N-alkylation of the sulfonamide moiety, in a group of arylsulfonamide derivatives of (aryloxy)ethyl piperidines, may be considered as a strategy for the design of selective 5-HT₇ receptor ligands or multifunctional agents to extend a polypharmacological approach to the treatment of complex diseases. The study allowed for the identification of 31 (1-methyl-N-{1-[2-(2-(t-butyl)phenoxy)ethyl]piperidin-4-yl}-N-cyclopropylmethyl-1H-pyrazole-4-sulfonamide),...

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Preliminary mutagenicity and genotoxicity evaluation of selected arylsulfonamide derivatives of (aryloxy)alkylamines with potential psychotropic properties

Beata Powroźnik, Karolina Słoczyńska, Vittorio Canale, Katarzyna Grychowska, more

Journal of Applied Genetics > 2016 > 57 > 2 > 263-270

Determination of the mutagenic and genotoxic liability of biologically active compounds is of great concern for preliminary toxicity testing and drug development. In this study, we focused on the evaluation of the mutagenic and genotoxic effects of selected arylsulfonamide derivatives of aryloxyethyl piperidines and pyrrolidines (1–8), classified as 5-HT₇ receptor antagonist with antidepressant and...

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Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols

Agnieszka Gunia-Krzyżak, Ewa Żesławska, Karolina Słoczyńska, Paulina Koczurkiewicz, more

European Journal of Medicinal Chemistry > 2016 > 107 > Complete > 26-37

Adequate control of seizures remains an unmet need in epilepsy. In order to identify new anticonvulsant agents, a series of N-trans-cinnamoyl derivatives of selected aminoalkanols was synthetized. The compounds were obtained in the reaction of N-acylation carried out in a two-phase system. The substances were tested in animal models of seizures induced either electrically (maximal electroshock – MES;...

article

Cardiovascular activity of the chiral xanthone derivatives

Natalia Szkaradek, Anna Rapacz, Karolina Pytka, Barbara Filipek, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 20 > 6714-6724

A series of 6 derivatives of xanthone were synthesized and evaluated for cardiovascular activity. The following pharmacological experiments were conducted: the binding affinity for adrenoceptors, the influence on the normal electrocardiogram, the effect on the arterial blood pressure, the effect on blood pressor response and prophylactic antiarrhythmic activity in adrenaline induced model of arrhythmia...

article

N-[(2,6-Dimethylphenoxy)alkyl]aminoalkanols—their physicochemical and anticonvulsant properties

Anna M. Waszkielewicz, Marek Cegła, Ewa Żesławska, Wojciech Nitek, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 15 > 4197-4217

Twenty four new N-[(dimethylphenoxy)alkyl]aminoalkanols have been synthesized and evaluated for anticonvulsant activity in a series of in vivo tests: the maximum electroshock (MES), 6Hz, and subcutaneous metrazole (ScMet). The compounds were also evaluated for possible neurotoxicity in the rotarod test. The majority of the achieved compounds exhibit quantified anticonvulsant activity. The most active...

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New Arylpiperazinylalkyl Derivatives of 8‐Alkoxy‐purine‐2,6‐dione and Dihydro[1,3]oxazolo[2,3‐f]purinedione Targeting the Serotonin 5‐HT_1A/5‐HT_2A/5‐HT₇ and Dopamine D₂ Receptors

Grażyna Chłoń‐Rzepa, Agnieszka Zagórska, Adam Bucki, Marcin Kołaczkowski, more

Archiv der Pharmazie > 348 > 4 > 242 - 253

To obtain potential antidepressants and/or antipsychotics, a series of new long‐chain arylpiperazine derivatives of 8‐alkoxy‐purine‐2,6‐dione (10–24) and dihydro[1,3]oxazolo[2,3‐f]purinedione (30–34) were synthesized and their serotonin (5‐HT_1A, 5‐HT_2A, 5‐HT₆, 5‐HT₇) and dopamine (D₂) receptor affinities were determined. The study allowed the identification of some potent 5‐HT_1A/5‐HT₇/D₂ ligands with...

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Skin metabolism established with the use of MetaSite for selected retinoids employed in topical and systemic treatment of various skin disorders and found in cosmeceuticals

Karolina Słoczyńska, Agnieszka Gunia-Krzyżak, Dorota Żelaszczyk, Anna Waszkielewicz, more

Acta Biochimica Polonica > 2015 > 62 > 2 > 201-206

Purpose. Besides being widely used in cosmetics, retinoids are potent therapeutic agents used topically and systemically as anti-acne agents. The aim of this study was to predict with the use of MetaSite the skin metabolism of selected retinoids employed in treatment of skin disorders and found in cosmeceuticals. The following compounds were studied: retinol, retinaldehyde, retinoic acid, retinyl...

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Preliminary assessment of mutagenic and anti-mutagenic potential of some aminoalkanolic derivatives of xanthone by use of the Vibrio harveyi assay

Karolina Słoczyńska, Anna Maria Waszkielewicz, Henryk Marona

Mutation Research - Genetic Toxicology and Environmental Mutagenesis > 2014 > 768 > Complete > 8-13

The Vibrio harveyi assay was used to evaluate mutagenic and anti-mutagenic effects of four new aminoalkanolic derivatives of xanthone with anticonvulsant activity, to select the potentially safe compounds for further in vivo studies in animal models.The study showed that at a concentration of 40ng/ml the test compounds were not mutagenic. Additionally, two of the investigated compounds, namely the...

article

Antimutagenic compounds and their possible mechanisms of action

Karolina Słoczyńska, Beata Powroźnik, Elżbieta Pękala, Anna M. Waszkielewicz

Journal of Applied Genetics > 2014 > 55 > 2 > 273-285

Mutagenicity refers to the induction of permanent changes in the DNA sequence of an organism, which may result in a heritable change in the characteristics of living systems. Antimutagenic agents are able to counteract the effects of mutagens. This group of agents includes both natural and synthetic compounds. Based on their mechanism of action among antimutagens, several classes of compounds may...

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In vitro effect of pentoxifylline and lisofylline on deformability and aggregation of red blood cells from healthy subjects and patients with chronic venous disease

Karolina Słoczyńska, Mariusz Kózka, Elżbieta Pękala, Anna Marchewka, more

Acta Biochimica Polonica > 2013 > 60 > 1 > 129-135

Purpose. The aim of the study was to assess the in vitro potency of pentoxifylline (PTX) and one of its most active metabolites lisofylline (LSF) to improve rheological properties of red blood cells (RBC) from healthy individuals and patients with chronic venous disease (CVD). Additionally, the study aimed to compare the effects of PTX and LSF on RBC deformability and aggregation. Methods. Blood samples...

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Keywords

MUTAGENICITY (5)
AMES TEST (3)
CRYSTAL STRUCTURE (3)
MES (3)
AMINOALKANOLS (2)
ANTICONVULSANT ACTIVITY (2)
ANTIMUTAGENICITY (2)
BIOTRANSFORMATION (2)
CINNAMAMIDE (2)
DEPRESSION (2)
SEIZURES (2)
XANTHONE (2)
SALMONELLA TYPHIMURIUM (TA1535/PSK1002) (1)
VIBRIO HARVEYI ASSAY (1)
5-HT7 RECEPTOR ANTAGONIST (1)
5-HT7 RECEPTOR ANTAGONISTS (1)
6-HZ (1)
6HZ (1)
9H‐XANTHEN‐9‐ONE (1)
ADRENOCEPTOR (1)
AGGREGATION (1)
ALTERNATIVE TEST (1)
ANTI-MUTAGENICITY (1)
ANTI/MUTAGENESIS (1)
ANTIARRHYTHMIC (1)
ANTICONVULSANT (1)
ANTIMUTAGEN (1)
ARYLPIPERAZINES (1)
BENZENESULFONAMIDE (1)
COGNITIVE DEFICITS (1)
CUNNINGHAMELLA (1)
CUNNINGHAMELLA ASSAY (1)
CYTOCHROME P450 (1)
DEFORMABILITY (1)
DNA DAMAGE (1)
DPPH ASSAY (1)
DSC (1)
GENOTOXICITY (1)
HEPATOTOXICITY (1)
HYPOTENSIVE (1)
LISOFYLLINE (1)
METABOLIC STABILITY (1)
METABOLISM (1)
METASITE (1)
MICROSOMAL STABILITY (1)
MICROSOMES (1)
MULTIMODAL 5-HT/DOPAMINE LIGANDS (1)
MUTAGEN (1)
N-ALKYLATED SULFONAMIDES (1)
PENTOXIFYLLINE (1)
PHARMACOPHORE (1)
PIPERAZINE DERIVATIVES (1)
RAT MICROSOMES (1)
RED BLOOD CELLS (1)
RETINOIDS (1)
ROTAROD (1)
SCPTZ (1)
SEROTONIN RECEPTOR LIGANDS (1)
SKIN METABOLISM (1)
SOS RESPONSE (1)
SOS/UMU-TEST (1)
STATUS EPILEPTICUS (1)
SYNTHESIS (1)
TG (1)
TOX (1)
VIBRIO HARVEYI (1)
XANTHONE DERIVATIVES (1)
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Elsevier (6)
Wiley (4)
Springer (3)
PSJD (2)

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Search results for: Karolina Słoczyńska

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