Search results for: Anna M. Waszkielewicz

Items from 1 to 15 out of 15 results

article

Promising anticonvulsant and/or analgesic compounds among 5‐chloro‐2‐ or 5‐chloro‐4‐methyl derivatives of xanthone coupled to aminoalkanol moieties—Design, synthesis and pharmacological evaluation

Gabriela Mazur, Katarzyna Pańczyk‐Straszak, Anna Rapacz, Jan Kiszela, more

Chemical Biology & Drug Design > 101 > 2 > 278 - 325

A series of 10 aminoalkanol derivatives of 5‐chloro‐2‐ or 5‐chloro‐4‐methylxanthone was synthetized and evaluated for anticonvulsant properties (MES test, mice, intraperitoneal) and compared with neurotoxicity rotarod test (NT, mice, i.p.). The best results both in terms of anticonvulsant activity and protective index value were obtained for 3: 5‐chloro‐2‐([4‐hydroxypiperidin‐1‐yl]methyl)‐9H‐xanthen‐9‐one...

article

Design, synthesis and activity against Staphylococcus epidermidis of 5‐chloro‐2‐ or 5‐chloro‐4‐methyl‐9H‐xanthen‐9‐one and some of its derivatives

Gabriela Mazur, Iwona Skiba‐Kurek, Elżbieta Karczewska, Katarzyna Pańczyk‐Straszak, more

Chemical Biology & Drug Design > 97 > 3 > 674 - 685

Ten new xanthone derivatives have been designed and synthesized for their potential antibacterial activity. All compounds have been screened against Staphylococcus epidermidis strains ATCC 12228 and clinical K/12/8915. The highest antibacterial activity was observed for compound 3: 5‐chloro‐2‐((4‐(2‐hydroxyethyl)piperazin‐1‐yl)methyl)‐9H‐xanthen‐9‐one dihydrochloride, exhibiting MIC of 0.8 µg/ml against...

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

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

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

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

Simultaneous LC/ESI‐MS Separation Method for the Enantioseparation of Some New Anticonvulsant Drugs

Maria Walczak, Elzbieta Pekala, Anna M. Waszkielewicz, Henryk Marona

Chirality > 26 > 3 > 144 - 149

A sensitive and specific method for the simultaneous determination of the enantiomeric purity of 2,6‐dimethylphenoxyacetyl derivatives as trans or cis racemic and enantiomeric forms with 2‐ or 4‐aminocyclohexanol moiety (1, 2, 3, 6) and their amine analogs (8, 9) was developed. The compounds studied are known for their anticonvulsant activity and the most interesting pharmacological results were those...

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...

article

Anticonvulsant evaluation of aminoalkanol derivatives of 2- and 4-methylxanthone

Natalia Szkaradek, Agnieszka Gunia, Anna M. Waszkielewicz, Lucyna Antkiewicz-Michaluk, more

Bioorganic & Medicinal Chemistry > 2013 > 21 > 5 > 1190-1198

A series of 17 new aminoalkanol derivatives of 6-methoxy- or 7-chloro-2-methylxanthone as well as 6-methoxy-4-methylxanthone was synthesized and evaluated for anticonvulsant activity. All compounds were verified in mice after intraperitoneal (ip) administration in maximal electroshock (MES) and subcutaneous pentetrazole (scMet) induced seizures as well as neurotoxicity assessment. Eleven of the tested...

article

Synthesis and anticonvulsant activity of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs

Elżbieta Pękala, Anna M. Waszkielewicz, Edward Szneler, Maria Walczak, more

Bioorganic & Medicinal Chemistry > 2011 > 19 > 22 > 6927-6934

A group of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2-hydroxycyclohexyl)acetamides (1–7) and -ethylamines (8–9) have been synthesized and investigated for their anticonvulsant activity. One of them, racemic trans-2-(2,6-dimethylphenoxy)-N-(2-hydroxycyclohexyl)acetamide proved to be the most effective in MES (mice, ip), exhibiting ED ₅₀ =42.97mg/kg b.w. and TD ₅₀ =105.67mg/kg b.w....

Filter options

Publication date

Last 3 years (1)

Close

Date range setting

Set the date range to filter the displayed results. You can set a starting date, ending date or both. You can enter the dates manually or choose them from the calendar.

From:

To:
Set your own date range

Keywords

Data set

Wiley (7)
Elsevier (6)
Springer (2)

Journal

Chemical Biology & Drug Design (5)
Bioorganic & Medicinal Chemistry (4)
Chirality (1)
European Journal of Medicinal Chemistry (1)
Investigational New Drugs (1)
Journal of Applied Genetics (1)
Journal of Biochemical and Molecular Toxicology (1)
Pharmacology Biochemistry and Behavior (1)

INFONA - science communication portal

Search results for: Anna M. Waszkielewicz

Add recipient

Sending message cancelled

Are you sure you want to cancel sending this message?

Send message

Filter options

Publication date

Date range setting

Set the date range to filter the displayed results. You can set a starting date, ending date or both. You can enter the dates manually or choose them from the calendar.

Keywords

Data set

Journal

Reporting an error / abuse

Sending the report failed

Accessibility options