Search results for: Henryk Marona

Items from 1 to 20 out of 31 results

article

Preliminary antifungal activity assay of selected chlorine‐containing derivatives of xanthone and phenoxyethyl amines

Karolina Klesiewicz, Dorota Żelaszczyk, Danuta Trojanowska, Bożena Bogusz, more

Chemical Biology & Drug Design > 92 > 5 > 1867 - 1875

The aim of this study was to evaluate antifungal activity in a diverse group of chlorine‐containing xanthone and phenoxyethyl amine derivatives – and to select the most promising compounds for further studies. The antifungal efficacy of 16 compounds was tested with qualitative and quantitative methods against both reference and clinical strains of dermatophytes, moulds and yeasts. The disc‐diffusion...

article

Contribution of reactive oxygen species to the anticancer activity of aminoalkanol derivatives of xanthone

Daniel Sypniewski, Natalia Szkaradek, Tomasz Loch, Anna M. Waszkielewicz, more

Investigational New Drugs > 2018 > 36 > 3 > 355-369

Summary Reactive oxygen species (ROS) are critically involved in the action of anticancer agents. In this study, we investigated the role of ROS in the anticancer mechanism of new aminoalkanol derivatives of xanthone. Most xanthones used in the study displayed significant pro-oxidant effects similar to those of gambogic acid, one of the most active anticancer xanthones. The pro-oxidant activity of...

article

Physicochemical and biological evaluation of a cinnamamide derivative R,S‐(2E)‐1‐(3‐hydroxypiperidin‐1‐yl)‐3‐phenylprop‐2‐en‐1‐one (KM‐608) for nervous system disorders

Agnieszka Gunia‐Krzyżak, Ewa Żesławska, Florence M. Bareyre, Wojciech Nitek, more

Chemical Biology & Drug Design > 90 > 2 > 244 - 253

A cinnamamide scaffold has been successfully incorporated in several compounds possessing desirable pharmacological activities in central and peripheral nervous system such as anticonvulsant, antidepressant, neuroprotective, analgesic, anti‐inflammatory, muscle relaxant, and sedative/hypnotic properties. R,S‐(2E)‐1‐(3‐hydroxypiperidin‐1‐yl)‐3‐phenylprop‐2‐en‐1‐one (KM‐608), a cinnamamide derivative,...

article

Evaluation of anti-inflammatory and ulcerogenic potential of zinc–ibuprofen and zinc–naproxen complexes in rats

Magdalena Jarosz, Natalia Szkaradek, Henryk Marona, Gabriel Nowak, more

Inflammopharmacology > 2017 > 25 > 6 > 653-663

Because of numerous indications and high availability, non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly prescribed and used medicines in the world. However, long-term therapy with and improper use of NSAIDs may lead to gastrointestinal damage. Therefore, improving the therapeutic index of the existing drugs has become a priority over the past decades. Considerable attention...

article

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...

article

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...

article

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...

article

HBK-7 — A new xanthone derivative and a 5-HT1A receptor antagonist with antidepressant-like properties

Karolina Pytka, Grzegorz Kazek, Agata Siwek, Barbara Mordyl, more

Pharmacology Biochemistry and Behavior > 2016 > 146-147 > C > 35-43

Xanthone derivatives possess many biological properties, including neuroprotective, antioxidant or antidepressant-like. In this study we aimed to investigate antidepressant- and anxiolytic-like properties of a new xanthone derivative – 6-methoxy-4-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one (HBK-7), as well as its possible mechanism of action, and the influence on cognitive and motor function...

article

Anticonvulsant Activity of Enantiomeric N‐trans‐Cinnamoyl Derivatives of 2‐Aminopropan‐1‐ols and 2‐Aminobutan‐1‐ols

Agnieszka Gunia‐Krzyżak, Ewa Żesławska, Wojciech Nitek, Justyna Popiół, more

Chirality > 28 > 6 > 482 - 488

Epilepsy, one of the most frequent neurological disorders, is still insufficiently treated in about 30% of patients. As a consequence, identification of novel anticonvulsant agents is an important issue in medicinal chemistry. In the present article we report synthesis, physicochemical, and pharmacological evaluation of N‐trans‐cinnamoyl derivatives of R and S‐2‐aminopropan‐1‐ol, as well as R and...

article

Antidepressant-like activity of aroxyalkyl derivatives of 2-methoxyphenylpiperazine and evidence for the involvement of serotonin receptor subtypes in their mechanism of action

Monika Kubacka, Szczepan Mogilski, Marek Bednarski, Leszek Nowiński, more

Pharmacology Biochemistry and Behavior > 2016 > 141 > C > 28-41

Since serotonin (5-HT) is strongly involved in the etiology and pathophysiology of depression, the development of new antidepressants is still based on the serotonergic system. The complexity of serotonergic system provides an opportunity for the development of compounds with multiple and complementary mechanism of action. This study describes serotonin receptor profile, functional characterization,...

article

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

The antidepressant-like activity of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one involves serotonergic 5-HT1A and 5-HT2A/C receptors activation

Karolina Pytka, Maria Walczak, Agnieszka Kij, Anna Rapacz, more

European Journal of Pharmacology > 2015 > 764 > Complete > 537-546

Xanthone derivatives have been shown to posses many biological properties. Some of them act within the central nervous system and show neuroprotective or antidepressant-like properties. Taking this into account we investigated antidepressant-like activity in mice and the possible mechanism of action of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one (HBK-11) – a new xanthone derivative...

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...

article

Synthesis and Evaluation of Antidepressant‐like Activity of Some 4‐Substituted 1‐(2‐methoxyphenyl)Piperazine Derivatives

Anna M. Waszkielewicz, Karolina Pytka, Anna Rapacz, Elżbieta Wełna, more

Chemical Biology & Drug Design > 85 > 3 > 326 - 335

A series of new derivatives of N‐(2‐methoxyphenyl)piperazine have been synthesized for their affinity toward serotonergic receptors and for their potential antidepressant‐like activity. They have been evaluated toward receptors 5‐HT_1A, 5‐HT₆, and 5‐HT₇, as well as in vivo in the tail suspension, locomotor activity, and motor co‐ordination tests. All the tested compounds proved very good affinities...

article

Synthesis, Anticonvulsant Activity and Metabolism of 4‐chlor‐3‐methylphenoxyethylamine Derivatives of Trans‐2‐aminocyclohexan‐1‐ol

Paulina Kubowicz, Henryk Marona, Elżbieta Pękala

Chirality > 27 > 2 > 163 - 169

In this study, we report the synthesis, spectral characterization, antiepileptic activity and biotransformation of three new, chiral, N‐aminoalkyl derivatives of trans – 2 aminocyclohexan‐1‐ol: 1 (R enantiomer), 2 (S enantiomer) and 3 (racemate). Antiepileptic activity of the titled compounds was studied using MES and scMet. Moreover, in this study, the biotransformation of 1, 2 and 3 in microbial...

article

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...

article

Antiarrhythmic activity of some xanthone derivatives with β1-adrenoceptor affinities in rats

Anna Rapacz, Jacek Sapa, Marek Bednarski, Barbara Filipek, more

European Journal of Pharmacology > 2014 > 738 > C > 14-21

A series of aminoalkanolic derivatives of xanthone with high affinity for β₁-adrenoceptors was evaluated for antiarrhythmic activity in the model of ischemia-reperfusion in isolated hearts, as well as in barium chloride- and adrenaline-induced model of arrhythmia. In order to better understand biological activity of studied compounds, the influence on β₂-adrenoceptors in guinea-pig trachea and vasorelaxant...

article

Antiarrhythmic, hypotensive and α1-adrenolytic properties of new 2-methoxyphenylpiperazine derivatives of xanthone

Anna Rapacz, Karolina Pytka, Jacek Sapa, Monika Kubacka, more

European Journal of Pharmacology > 2014 > 735 > Complete > 10-16

The main goal of this study was to assess antiarrhythmic and hypotensive activity of new 2-methoxyphenylpiperazine derivatives of xanthone. In order to better understand mechanism of action of studied compounds, their abilities to antagonize the increase in blood pressure elicited by adrenaline, noradrenaline and methoxamine, as well as the antagonistic properties for α ₁ -adrenoceptors on...

article

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...

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Search results for: Henryk Marona

Preliminary antifungal activity assay of selected chlorine‐containing derivatives of xanthone and phenoxyethyl amines

Contribution of reactive oxygen species to the anticancer activity of aminoalkanol derivatives of xanthone

Physicochemical and biological evaluation of a cinnamamide derivative R,S‐(2E)‐1‐(3‐hydroxypiperidin‐1‐yl)‐3‐phenylprop‐2‐en‐1‐one (KM‐608) for nervous system disorders

Evaluation of anti-inflammatory and ulcerogenic potential of zinc–ibuprofen and zinc–naproxen complexes in rats

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

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

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

HBK-7 — A new xanthone derivative and a 5-HT1A receptor antagonist with antidepressant-like properties

Anticonvulsant Activity of Enantiomeric N‐trans‐Cinnamoyl Derivatives of 2‐Aminopropan‐1‐ols and 2‐Aminobutan‐1‐ols

Antidepressant-like activity of aroxyalkyl derivatives of 2-methoxyphenylpiperazine and evidence for the involvement of serotonin receptor subtypes in their mechanism of action

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

Cardiovascular activity of the chiral xanthone derivatives

The antidepressant-like activity of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one involves serotonergic 5-HT1A and 5-HT2A/C receptors activation

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

Synthesis and Evaluation of Antidepressant‐like Activity of Some 4‐Substituted 1‐(2‐methoxyphenyl)Piperazine Derivatives

Synthesis, Anticonvulsant Activity and Metabolism of 4‐chlor‐3‐methylphenoxyethylamine Derivatives of Trans‐2‐aminocyclohexan‐1‐ol

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

Antiarrhythmic activity of some xanthone derivatives with β1-adrenoceptor affinities in rats

Antiarrhythmic, hypotensive and α1-adrenolytic properties of new 2-methoxyphenylpiperazine derivatives of xanthone

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

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