Search results for: Katarzyna Kieć-Kononowicz

Items from 1 to 20 out of 79 results

article

Novel selective agonist of GPR18, PSB‐KK‐1415 exerts potent anti‐inflammatory and anti‐nociceptive activities in animal models of intestinal inflammation and inflammatory pain

Adam Fabisiak, Natalia Fabisiak, Anna Mokrowiecka, Ewa Malecka‐Panas, more

Neurogastroenterology & Motility > 33 > 3 > n/a - n/a

Background GPR18 is a recently deorphanized receptor which was reported to act with several endogenous cannabinoid ligands. Here, we aimed to describe the role of GPR18 in intestinal inflammation and inflammatory pain. Methods The anti‐inflammatory activity of selective GPR18 agonist, PSB‐KK‐1415, and antagonist, PSB‐CB5, was characterized in semi‐chronic and chronic mouse models of colitis induced...

article

Structure-activity relationships of imidazothiazinones and analogs as antagonists of the cannabinoid-activated orphan G protein-coupled receptor GPR18

Clara T. Schoeder, Maria Kaleta, Andhika B. Mahardhika, Agnieszka Olejarz-Maciej, more

European Journal of Medicinal Chemistry > 2018 > 155 > C > 381-397

GPR18 is a cannabinoid-activated orphan G protein-coupled receptor (GPCR) that is selectively expressed on immune cells. Despite its significant potential as a drug target for inflammatory diseases and cancer immunotherapy, only very few GPR18 ligands have been described to date. In the present study we investigated the structure-activity relationships (SARs) of (Z)-2-(3-(4-chlorobenzyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one...

article

Antinociceptive effects of novel histamine H₃ and H₄ receptor antagonists and their influence on morphine analgesia of neuropathic pain in the mouse

Katarzyna Popiolek‐Barczyk, Dorota Łażewska, Gniewomir Latacz, Agnieszka Olejarz, more

British Journal of Pharmacology > 175 > 14 > 2897 - 2910

Background and Purpose The histaminergic system is a promising target for the development of new analgesics, as histamine H₃ and H₄ receptors are expressed in regions concerned with nociceptive transmission. Here we have determined the analgesic effects of new H₃ and H₄ receptor antagonists in naive and neuropathic mice. Experimental Approach We used chronic constriction injury (CCI) to the sciatic...

article

The histamine H₃ receptor inverse agonist pitolisant reduces body weight in obese mice

Magdalena Kotańska, Kamil J. Kuder, Katarzyna Szczepańska, Jacek Sapa, more

Naunyn-Schmiedeberg's Archives of Pharmacology > 2018 > 391 > 8 > 875-881

The pharmacological profile of pitolisant, a histamine H₃ receptor antagonist/inverse agonist, indicates that this compound might reduce body weight and metabolic disturbances. Therefore, we studied the influence of pitolisant on body weight, water and sucrose intake as well as metabolic disturbances in the high-fat and high-sugar diet-induced obesity model in mice. To induce obesity, male CD-1 mice...

article

Phenylalanine derivatives with modulating effects on human α1-glycine receptors and anticonvulsant activity in strychnine-induced seizure model in male adult rats

Bassem Sadek, Murat Oz, Syed M. Nurulain, Petrilla Jayaprakash, more

Epilepsy Research > 2017 > 138 > C > 124-131

The critical role of α1-glycine receptor (α1-GLYRs) in pathological conditions such as epilepsy is well known. In the present study, structure-activity relations for a series of phenylalanine derivatives carrying selected hydrogen bond acceptors were investigated on the functional properties of human α1-GLYR expressed in Xenopus oocytes. The results indicate that one particular substitution position...

article

Aryl‐ and heteroaryl‐substituted phenylalanines as AMPA receptor ligands

Ewa Szymańska, Paulina Chałupnik, Tommy N. Johansen, Birgitte Nielsen, more

Chemical Biology & Drug Design > 90 > 6 > 1271 - 1281

A series of racemic unnatural amino acids was rationally designed on the basis of recently published X‐ray structures of the GluA2 LBD with bound phenylalanine‐based antagonists. Twelve new diaryl‐ or aryl/heteroaryl‐substituted phenylalanine derivatives were synthesized and evaluated in vitro in radioligand binding assays at native rat ionotropic glutamate receptors. The most interesting compound...

article

In the search for a lead structure among series of potent and selective hydantoin 5‐HT₇R agents: The drug‐likeness in vitro study

Gniewomir Latacz, Annamaria Lubelska, Magdalena Jastrzębska‐Więsek, Anna Partyka, more

Chemical Biology & Drug Design > 90 > 6 > 1295 - 1306

Since the year 1993, when 5‐HT₇ receptor (5‐HT₇R) was discovered, there is no selective 5‐HT₇R ligand introduced to the pharmaceutical market. One out of the main reasons disqualifying the 5‐HT₇R ligands is weak drugability properties, including metabolic instability or low permeability. This study is focused on the search of a lead compound by “drug‐likeness” estimation of the first series of selective...

article

Study on the effect of EMD386088, a 5-HT₆ receptor partial agonist, in enhancing the anti-immobility action of some antidepressants in rats

Magdalena Jastrzębska-Więsek, Agata Siwek, Anna Partyka, Marcin Kołaczkowski, more

Naunyn-Schmiedeberg's Archives of Pharmacology > 2018 > 391 > 1 > 37-49

The effect of some antidepressants co-administered with EMD386088 in the modified forced swim test in rats was investigated. Additionally, the pharmacokinetics, metabolic stability, and the effect of EMD386088 on P450 cytochromes were determined. Intraperitoneal (i.p.) coadministration of EMD386088 (2.5 mg/kg) and imipramine (15 mg/kg), reboxetine (5 mg/kg), moclobemide (10 mg/kg), or bupropion (10 mg/kg)...

article

Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands

Dorota Łażewska, Maria Kaleta, J. Stephan Schwed, Tadeusz Karcz, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 20 > 5341-5354

Novel biphenyloxy-alkyl derivatives of piperidine and azepane were synthesized and evaluated for their binding properties at the human histamine H₃ receptor. Two series of compounds were obtained with a meta- and a para-biphenyl moiety. The alkyl chain spacer contained five and six carbon atoms. The highest affinity among all compounds was shown by 1-(6-(3-phenylphenoxy)hexyl)azepane (13) with a K...

article

Spectroscopic investigations of novel pharmaceuticals: Stability and resonant interaction with laser beam

Adriana Smarandache, Mihai Boni, Ionut Relu Andrei, Jadwiga Handzlik, more

Applied Surface Science > 2017 > 417 > C > 143-148

This paper presents data about photophysics of two novel thio-hydantoins that exhibit promising pharmaceutical properties in multidrug resistance control. Time stability studies are necessary to establish the proper use of these compounds in different applications. As for their administration as drugs, it is imperative to know their shelf life, as well as storage conditions.At the same time, laser...

article

Pharmacological characterization and binding modes of novel racemic and optically active phenylalanine-based antagonists of AMPA receptors

Ewa Szymańska, Birgitte Nielsen, Tommy N. Johansen, Ana Maria Cuñado Moral, more

European Journal of Medicinal Chemistry > 2017 > 138 > C > 874-883

In order to map out molecular determinants for the competitive blockade of AMPA receptor subtypes, a series of racemic aryl-substituted phenylalanines was synthesized and pharmacologically characterized in vitro at native rat ionotropic glutamate receptors. Most of the compounds showed micromolar affinity and preference for AMPA receptors. Individual stereoisomers of selected compounds were further...

article

The computer-aided discovery of novel family of the 5-HT6 serotonin receptor ligands among derivatives of 4-benzyl-1,3,5-triazine

Dorota Łażewska, Rafał Kurczab, Małgorzata Więcek, Katarzyna Kamińska, more

European Journal of Medicinal Chemistry > 2017 > 135 > C > 117-124

The work describes a discovery of new chemical family of potent ligands for the 5-HT₆ serotonin receptors. During the search for new histamine H₄ receptor antagonists among 1,3,5-triazine derivatives, compound 2 (4-benzyl-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) was found. Compound 2, weakly active for the H₄ receptor but fitted in 3/4 of pharmacophore features of the 5-HT₆R ligand, occurred...

article

Synthesis and biological activity of novel tert-amylphenoxyalkyl (homo)piperidine derivatives as histamine H3R ligands

Kamil J. Kuder, Dorota Łażewska, Maria Kaleta, Gniewomir Latacz, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 10 > 2701-2712

As a continuation of our search for novel histamine H₃ receptor ligands a series of twenty new tert-amyl phenoxyalkylamine derivatives (2–21) was synthesized. Compounds of four to eight carbon atoms spacer alkyl chain were evaluated on their binding properties at human histamine H₃ receptor (hH₃R). The highest affinities were observed for pentyl derivatives 6–8 (K_i=8.8–23.4nM range) and among them...

article

Natural selenium particles from Staphylococcus carnosus: Hazards or particles with particular promise?

Ethiene Castellucci Estevam, Sharoon Griffin, Muhammad Jawad Nasim, Polina Denezhkin, more

Journal of Hazardous Materials > 2017 > 324 > PA > 22-30

Various bacteria, including diverse Staphylococci, reduce selenite to yield red selenium particles with diameters in the high nanometer to low micrometer range. Formation and accumulation of such particles in bacteria often results in cell death, triggered by a loss of thiols and formation of disruptive deposits inside the cell. Hence certain pathogenic bacteria are rather sensitive to the presence...

article

Design, synthesis and structure–activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands

Ewa Szymańska, Paulina Chałupnik, Katarzyna Szczepańska, Ana Maria Cuñado Moral, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 22 > 5568-5572

A new series of carboxyaryl-substituted phenylalanines was designed, synthesized and pharmacologically characterized in vitro at native rat ionotropic glutamate receptors as well as at cloned homomeric kainate receptors GluK1–GluK3. Among them, six compounds bound to GluK1 receptor subtypes with reasonable affinity (K_i values in the range of 4.9–7.5μM). A structure–activity relationship (SAR) for...

article

Aryl-1,3,5-triazine ligands of histamine H₄ receptor attenuate inflammatory and nociceptive response to carrageen, zymosan and lipopolysaccharide

Szczepan Mogilski, Monika Kubacka, Dorota Łażewska, Małgorzata Więcek, more

Inflammation Research > 2017 > 66 > 1 > 79-95

Objective and design Histamine H₄ receptor (H₄R) offers a great potential for new therapeutic strategies for the treatment of inflammation-based diseases. The aim of this study is to present the pharmacological profile of two recently synthesized ligands of H₄R with particular reference to their anti-inflammatory and analgesic activity. Materials and subjects We used mice and rats in the in vivo...

article

Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors

Ewa Szymańska, Anna Drabczyńska, Tadeusz Karcz, Christa E. Müller, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 18 > 4347-4362

A new series of 32 pyrimido- and 5 tetrahydropyrazino[2,1-f]purinediones was obtained and evaluated for their adenosine receptors (ARs) affinities. The 1,3-dibutyl derivative of 9-(4-(2-(dimethylamino)ethoxy)phenyl)-6,7,8,9-tetrahydropyrimido[1,2-f]purine-2,4(1H,3H)-dione was found to be the most potent A₁ AR antagonist of the present series, showing selectivity over the other AR subtypes. The structure–activity...

article

Cholinesterase inhibitory activity of chlorophenoxy derivatives—Histamine H3 receptor ligands

Dorota Łażewska, Jakub Jończyk, Marek Bajda, Natalia Szałaj, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 16 > 4140-4145

In recent years, multitarget-directed ligands have become an interesting strategy in a search for a new treatment of Alzheimer’s disease. Combination of both: a histamine H₃ receptor antagonist/inverse agonist and a cholinesterases inhibitor in one molecule could provide a new therapeutic opportunity. Here, we present biological evaluation of histamine H₃ receptor ligands—chlorophenoxyalkylamine derivatives...

article

The Synthesis of 1,3,5‐triazine Derivatives and JNJ7777120 Analogues with Histamine H₄ Receptor Affinity and Their Interaction with PTEN Promoter

Gniewomir Latacz, Petros Kechagioglou, Rigini Papi, Dorota Łażewska, more

Chemical Biology & Drug Design > 88 > 2 > 254 - 263

The involvement of histamine and H₄ receptor (H₄R) in cancer has been investigated recently using the H₄R agonists and antagonists. The scope of the research project was synthesis and exploration of the consequences of a group of compounds with histamine H₄ receptor (H₄R) affinity on the promoter of PTEN gene encoding the antitumor PTEN protein. The series of novel compounds based either on H₄R antagonists...

article

The 5-aromatic hydantoin-3-acetate derivatives as inhibitors of the tumour multidrug resistance efflux pump P-glycoprotein (ABCB1): Synthesis, crystallographic and biological studies

Ewa Żesławska, Annamária Kincses, Gabriella Spengler, Wojciech Nitek, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 12 > 2815-2822

A series of arylpiperazine derivatives of hydantoin-3-acetate, including previously obtained 5,5-diphenylhydantoin (1–7) and new-synthesized spirofluorene-hydantoin derivatives (8–12), were investigated in the search for new inhibitors of the tumour multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp, ABCB1) overexpressed in mouse T-lymphoma cells. Synthesis of new compounds (8–12) was performed...

Publication date

Set your own date range

INFONA - science communication portal

Search results for: Katarzyna Kieć-Kononowicz

Novel selective agonist of GPR18, PSB‐KK‐1415 exerts potent anti‐inflammatory and anti‐nociceptive activities in animal models of intestinal inflammation and inflammatory pain

Structure-activity relationships of imidazothiazinones and analogs as antagonists of the cannabinoid-activated orphan G protein-coupled receptor GPR18

Antinociceptive effects of novel histamine H₃ and H₄ receptor antagonists and their influence on morphine analgesia of neuropathic pain in the mouse

The histamine H₃ receptor inverse agonist pitolisant reduces body weight in obese mice

Phenylalanine derivatives with modulating effects on human α1-glycine receptors and anticonvulsant activity in strychnine-induced seizure model in male adult rats

Aryl‐ and heteroaryl‐substituted phenylalanines as AMPA receptor ligands

In the search for a lead structure among series of potent and selective hydantoin 5‐HT₇R agents: The drug‐likeness in vitro study

Study on the effect of EMD386088, a 5-HT₆ receptor partial agonist, in enhancing the anti-immobility action of some antidepressants in rats

Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands

Spectroscopic investigations of novel pharmaceuticals: Stability and resonant interaction with laser beam

Pharmacological characterization and binding modes of novel racemic and optically active phenylalanine-based antagonists of AMPA receptors

The computer-aided discovery of novel family of the 5-HT6 serotonin receptor ligands among derivatives of 4-benzyl-1,3,5-triazine

Synthesis and biological activity of novel tert-amylphenoxyalkyl (homo)piperidine derivatives as histamine H3R ligands

Natural selenium particles from Staphylococcus carnosus: Hazards or particles with particular promise?

Design, synthesis and structure–activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands

Aryl-1,3,5-triazine ligands of histamine H₄ receptor attenuate inflammatory and nociceptive response to carrageen, zymosan and lipopolysaccharide

Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors

Cholinesterase inhibitory activity of chlorophenoxy derivatives—Histamine H3 receptor ligands

The Synthesis of 1,3,5‐triazine Derivatives and JNJ7777120 Analogues with Histamine H₄ Receptor Affinity and Their Interaction with PTEN Promoter

The 5-aromatic hydantoin-3-acetate derivatives as inhibitors of the tumour multidrug resistance efflux pump P-glycoprotein (ABCB1): Synthesis, crystallographic and biological studies

Filter options

Publication date

Keywords

Data set

Journal

INFONA - science communication portal

Search results for: Katarzyna Kieć-Kononowicz

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