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Items: 1 to 50 of 188

1.

Influence of the Novel Histamine H3 Receptor Antagonist/Inverse Agonist M39 on Gastroprotection and PGE2 Production Induced by (R)-Alpha-Methylhistamine in C57BL/6 Mice.

Bastaki SMA, Amir N, Więcek M, Kieć-Kononowicz K, Sadek B.

Front Pharmacol. 2019 Sep 12;10:966. doi: 10.3389/fphar.2019.00966. eCollection 2019.

2.

The dual-active histamine H3 receptor antagonist and acetylcholine esterase inhibitor E100 ameliorates stereotyped repetitive behavior and neuroinflammmation in sodium valproate induced autism in mice.

Eissa N, Azimullah S, Jayaprakash P, Jayaraj RL, Reiner D, Ojha SK, Beiram R, Stark H, Łażewska D, Kieć-Kononowicz K, Sadek B.

Chem Biol Interact. 2019 Oct 1;312:108775. doi: 10.1016/j.cbi.2019.108775. Epub 2019 Jul 30.

PMID:
31369746
3.

Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands.

Szczepańska K, Karcz T, Siwek A, Kuder KJ, Latacz G, Bednarski M, Szafarz M, Hagenow S, Lubelska A, Olejarz-Maciej A, Sobolewski M, Mika K, Kotańska M, Stark H, Kieć-Kononowicz K.

Bioorg Chem. 2019 Oct;91:103071. doi: 10.1016/j.bioorg.2019.103071. Epub 2019 Jun 20.

PMID:
31362197
4.

The 1,3,5-Triazine Derivatives as Innovative Chemical Family of 5-HT6 Serotonin Receptor Agents with Therapeutic Perspectives for Cognitive Impairment.

Latacz G, Lubelska A, Jastrzębska-Więsek M, Partyka A, Marć MA, Satała G, Wilczyńska D, Kotańska M, Więcek M, Kamińska K, Wesołowska A, Kieć-Kononowicz K, Handzlik J.

Int J Mol Sci. 2019 Jul 12;20(14). pii: E3420. doi: 10.3390/ijms20143420.

5.

KSK19 - Novel histamine H3 receptor ligand reduces body weight in diet induced obese mice.

Kotańska M, Mika K, Reguła K, Szczepańska K, Szafarz M, Bednarski M, Olejarz-Maciej A, Nowak K, Latacz G, Mogilski S, Kuder KJ, Kieć-Kononowicz K, Sapa J.

Biochem Pharmacol. 2019 Oct;168:193-203. doi: 10.1016/j.bcp.2019.07.006. Epub 2019 Jul 8.

PMID:
31295465
6.

Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT6.

Ali W, Więcek M, Łażewska D, Kurczab R, Jastrzębska-Więsek M, Satała G, Kucwaj-Brysz K, Lubelska A, Głuch-Lutwin M, Mordyl B, Siwek A, Nasim MJ, Partyka A, Sudoł S, Latacz G, Wesołowska A, Kieć-Kononowicz K, Handzlik J.

Eur J Med Chem. 2019 Sep 15;178:740-751. doi: 10.1016/j.ejmech.2019.06.022. Epub 2019 Jun 10.

PMID:
31229876
7.

Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors.

Mosolygó T, Kincses A, Csonka A, Tönki ÁS, Witek K, Sanmartín C, Marć MA, Handzlik J, Kieć-Kononowicz K, Domínguez-Álvarez E, Spengler G.

Molecules. 2019 Apr 16;24(8). pii: E1487. doi: 10.3390/molecules24081487.

8.

Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT7 receptor low-basicity agonists, potential neuropathic painkillers.

Hogendorf AS, Hogendorf A, Popiołek-Barczyk K, Ciechanowska A, Mika J, Satała G, Walczak M, Latacz G, Handzlik J, Kieć-Kononowicz K, Ponimaskin E, Schade S, Zeug A, Bijata M, Kubicki M, Kurczab R, Lenda T, Staroń J, Bugno R, Duszyńska B, Pilarski B, Bojarski AJ.

Eur J Med Chem. 2019 May 15;170:261-275. doi: 10.1016/j.ejmech.2019.03.017. Epub 2019 Mar 11.

PMID:
30904783
9.

Design, synthesis, and in vitro and in vivo characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H3 receptor antagonists.

Staszewski M, Stasiak A, Karcz T, McNaught Flores D, Fogel WA, Kieć-Kononowicz K, Leurs R, Walczyński K.

Medchemcomm. 2019 Jan 11;10(2):234-251. doi: 10.1039/c8md00527c. eCollection 2019 Feb 1.

PMID:
30881612
10.

Histamine H3 receptor antagonist E177 attenuates amnesia induced by dizocilpine without modulation of anxiety-like behaviors in rats.

Alachkar A, Khan N, Łażewska D, Kieć-Kononowicz K, Sadek B.

Neuropsychiatr Dis Treat. 2019 Feb 20;15:531-542. doi: 10.2147/NDT.S193125. eCollection 2019.

11.

Role of Histamine H₃ Receptor Antagonists on Intraocular Pressure Reduction in Rabbit Models of Transient Ocular Hypertension and Glaucoma.

Lanzi C, Lucarini L, Durante M, Sgambellone S, Pini A, Catarinicchia S, Łażewska D, Kieć-Kononowicz K, Stark H, Masini E.

Int J Mol Sci. 2019 Feb 24;20(4). pii: E981. doi: 10.3390/ijms20040981.

12.

Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.

Załuski M, Schabikowski J, Schlenk M, Olejarz-Maciej A, Kubas B, Karcz T, Kuder K, Latacz G, Zygmunt M, Synak D, Hinz S, Müller CE, Kieć-Kononowicz K.

Bioorg Med Chem. 2019 Apr 1;27(7):1195-1210. doi: 10.1016/j.bmc.2019.02.004. Epub 2019 Feb 2.

PMID:
30808606
13.

Alkyl derivatives of 1,3,5-triazine as histamine H4 receptor ligands.

Łażewska D, Mogilski S, Hagenow S, Kuder K, Głuch-Lutwin M, Siwek A, Więcek M, Kaleta M, Seibel U, Buschauer A, Filipek B, Stark H, Kieć-Kononowicz K.

Bioorg Med Chem. 2019 Apr 1;27(7):1254-1262. doi: 10.1016/j.bmc.2019.02.020. Epub 2019 Feb 12.

PMID:
30792106
14.

5-Arylideneimidazolones with Amine at Position 3 as Potential Antibiotic Adjuvants against Multidrug Resistant Bacteria.

Kaczor A, Witek K, Podlewska S, Czekajewska J, Lubelska A, Żesławska E, Nitek W, Latacz G, Alibert S, Pagès JM, Karczewska E, Kieć-Kononowicz K, Handzlik J.

Molecules. 2019 Jan 26;24(3). pii: E438. doi: 10.3390/molecules24030438.

15.

Search for a 5-CT alternative. In vitro and in vivo evaluation of novel pharmacological tools: 3-(1-alkyl-1H-imidazol-5-yl)-1H-indole-5-carboxamides, low-basicity 5-HT7 receptor agonists.

Latacz G, Hogendorf AS, Hogendorf A, Lubelska A, Wierońska JM, Woźniak M, Cieślik P, Kieć-Kononowicz K, Handzlik J, Bojarski AJ.

Medchemcomm. 2018 Sep 25;9(11):1882-1890. doi: 10.1039/c8md00313k. eCollection 2018 Nov 1.

16.

Synthesis and computer-aided analysis of the role of linker for novel ligands of the 5-HT6 serotonin receptor among substituted 1,3,5-triazinylpiperazines.

Łażewska D, Kurczab R, Więcek M, Satała G, Kieć-Kononowicz K, Handzlik J.

Bioorg Chem. 2019 Mar;84:319-325. doi: 10.1016/j.bioorg.2018.11.046. Epub 2018 Nov 26.

PMID:
30530073
17.

Optimization and preclinical evaluation of novel histamine H3receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives.

Szczepańska K, Karcz T, Kotańska M, Siwek A, Kuder KJ, Latacz G, Mogilski S, Hagenow S, Lubelska A, Sobolewski M, Stark H, Kieć-Kononowicz K.

Bioorg Med Chem. 2018 Dec 15;26(23-24):6056-6066. doi: 10.1016/j.bmc.2018.11.010. Epub 2018 Nov 10.

PMID:
30448256
18.

4-tert-Pentylphenoxyalkyl derivatives - Histamine H3 receptor ligands and monoamine oxidase B inhibitors.

Łażewska D, Olejarz-Maciej A, Kaleta M, Bajda M, Siwek A, Karcz T, Doroz-Płonka A, Cichoń U, Kuder K, Kieć-Kononowicz K.

Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3596-3600. doi: 10.1016/j.bmcl.2018.10.048. Epub 2018 Oct 31.

PMID:
30404719
19.

Studies on Anticonvulsant Effects of Novel Histamine H3R Antagonists in Electrically and Chemically Induced Seizures in Rats.

Alachkar A, Łażewska D, Latacz G, Frank A, Siwek A, Lubelska A, Honkisz-Orzechowska E, Handzlik J, Stark H, Kieć-Kononowicz K, Sadek B.

Int J Mol Sci. 2018 Oct 29;19(11). pii: E3386. doi: 10.3390/ijms19113386.

20.

Computer-Aided Studies for Novel Arylhydantoin 1,3,5-Triazine Derivatives as 5-HT₆ Serotonin Receptor Ligands with Antidepressive-Like, Anxiolytic and Antiobesity Action In Vivo.

Kurczab R, Ali W, Łażewska D, Kotańska M, Jastrzębska-Więsek M, Satała G, Więcek M, Lubelska A, Latacz G, Partyka A, Starek M, Dąbrowska M, Wesołowska A, Jacob C, Kieć-Kononowicz K, Handzlik J.

Molecules. 2018 Oct 3;23(10). pii: E2529. doi: 10.3390/molecules23102529.

21.

The histamine H3R antagonist DL77 attenuates autistic behaviors in a prenatal valproic acid-induced mouse model of autism.

Eissa N, Jayaprakash P, Azimullah S, Ojha SK, Al-Houqani M, Jalal FY, Łażewska D, Kieć-Kononowicz K, Sadek B.

Sci Rep. 2018 Aug 30;8(1):13077. doi: 10.1038/s41598-018-31385-7.

22.

The role of aryl-topology in balancing between selective and dual 5-HT7R/5-HT1A actions of 3,5-substituted hydantoins.

Kucwaj-Brysz K, Kurczab R, Żesławska E, Lubelska A, Marć MA, Latacz G, Satała G, Nitek W, Kieć-Kononowicz K, Handzlik J.

Medchemcomm. 2018 May 8;9(6):1033-1044. doi: 10.1039/c8md00168e. eCollection 2018 Jun 1.

23.

Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.

Załuski M, Stanuch K, Karcz T, Hinz S, Latacz G, Szymańska E, Schabikowski J, Doroż-Płonka A, Handzlik J, Drabczyńska A, Müller CE, Kieć-Kononowicz K.

Medchemcomm. 2018 May 14;9(6):951-962. doi: 10.1039/c8md00070k. eCollection 2018 Jun 1.

24.

2-Phenylquinoline S. aureus NorA Efflux Pump Inhibitors: Evaluation of the Importance of Methoxy Group Introduction.

Felicetti T, Cannalire R, Pietrella D, Latacz G, Lubelska A, Manfroni G, Barreca ML, Massari S, Tabarrini O, Kieć-Kononowicz K, Schindler BD, Kaatz GW, Cecchetti V, Sabatini S.

J Med Chem. 2018 Sep 13;61(17):7827-7848. doi: 10.1021/acs.jmedchem.8b00791. Epub 2018 Aug 17.

PMID:
30067360
25.

Probing Substituents in the 1- and 3-Position: Tetrahydropyrazino-Annelated Water-Soluble Xanthine Derivatives as Multi-Target Drugs With Potent Adenosine Receptor Antagonistic Activity.

Koch P, Brunschweiger A, Namasivayam V, Ullrich S, Maruca A, Lazzaretto B, Küppers P, Hinz S, Hockemeyer J, Wiese M, Heer J, Alcaro S, Kiec-Kononowicz K, Müller CE.

Front Chem. 2018 Jun 26;6:206. doi: 10.3389/fchem.2018.00206. eCollection 2018.

26.

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

Schoeder CT, Kaleta M, Mahardhika AB, Olejarz-Maciej A, Łażewska D, Kieć-Kononowicz K, Müller CE.

Eur J Med Chem. 2018 Jul 15;155:381-397. doi: 10.1016/j.ejmech.2018.05.050. Epub 2018 Jun 1.

PMID:
29902723
27.

Molecular and functional interaction between GPR18 and cannabinoid CB2 G-protein-coupled receptors. Relevance in neurodegenerative diseases.

Reyes-Resina I, Navarro G, Aguinaga D, Canela EI, Schoeder CT, Załuski M, Kieć-Kononowicz K, Saura CA, Müller CE, Franco R.

Biochem Pharmacol. 2018 Nov;157:169-179. doi: 10.1016/j.bcp.2018.06.001. Epub 2018 Jun 2.

28.

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

Kotańska M, Kuder KJ, Szczepańska K, Sapa J, Kieć-Kononowicz K.

Naunyn Schmiedebergs Arch Pharmacol. 2018 Aug;391(8):875-881. doi: 10.1007/s00210-018-1516-2. Epub 2018 May 25.

29.

Anticonvulsant evaluation of novel non-imidazole histamine H3R antagonists in different convulsion models in rats.

Alachkar A, Latacz G, Siwek A, Lubelska A, Honkisz E, Gryboś A, Łażewska D, Handzlik J, Stark H, Kiec-Kononowicz K, Sadek B.

Pharmacol Biochem Behav. 2018 Jul;170:14-24. doi: 10.1016/j.pbb.2018.04.010. Epub 2018 May 3.

PMID:
29729290
30.

Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands.

Szczepańska K, Karcz T, Mogilski S, Siwek A, Kuder KJ, Latacz G, Kubacka M, Hagenow S, Lubelska A, Olejarz A, Kotańska M, Sadek B, Stark H, Kieć-Kononowicz K.

Eur J Med Chem. 2018 May 25;152:223-234. doi: 10.1016/j.ejmech.2018.04.043. Epub 2018 Apr 25.

PMID:
29723785
31.

Novel naphthyloxy derivatives - Potent histamine H3 receptor ligands. Synthesis and pharmacological evaluation.

Łażewska D, Kaleta M, Hagenow S, Mogilski S, Latacz G, Karcz T, Lubelska A, Honkisz E, Handzlik J, Reiner D, Satała G, Filipek B, Stark H, Kieć-Kononowicz K.

Bioorg Med Chem. 2018 May 15;26(9):2573-2585. doi: 10.1016/j.bmc.2018.04.023. Epub 2018 Apr 11.

PMID:
29681486
32.

Fluorescent-Labeled Selective Adenosine A2B Receptor Antagonist Enables Competition Binding Assay by Flow Cytometry.

Köse M, Gollos S, Karcz T, Fiene A, Heisig F, Behrenswerth A, Kieć-Kononowicz K, Namasivayam V, Müller CE.

J Med Chem. 2018 May 24;61(10):4301-4316. doi: 10.1021/acs.jmedchem.7b01627. Epub 2018 May 15.

PMID:
29681156
33.

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

Popiolek-Barczyk K, Łażewska D, Latacz G, Olejarz A, Makuch W, Stark H, Kieć-Kononowicz K, Mika J.

Br J Pharmacol. 2018 Jul;175(14):2897-2910. doi: 10.1111/bph.14185. Epub 2018 May 31.

34.

The Histamine H3 Receptor Antagonist DL77 Ameliorates MK801-Induced Memory Deficits in Rats.

Eissa N, Khan N, Ojha SK, Łazewska D, Kieć-Kononowicz K, Sadek B.

Front Neurosci. 2018 Feb 12;12:42. doi: 10.3389/fnins.2018.00042. eCollection 2018.

35.

MF-8, a novel promising arylpiperazine-hydantoin based 5-HT7 receptor antagonist: In vitro drug-likeness studies and in vivo pharmacological evaluation.

Latacz G, Lubelska A, Jastrzębska-Więsek M, Partyka A, Kucwaj-Brysz K, Wesołowska A, Kieć-Kononowicz K, Handzlik J.

Bioorg Med Chem Lett. 2018 Mar 1;28(5):878-883. doi: 10.1016/j.bmcl.2018.02.003. Epub 2018 Feb 3.

PMID:
29439902
36.

Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT7 receptor agents with antidepressant activity.

Kucwaj-Brysz K, Kurczab R, Jastrzębska-Więsek M, Żesławska E, Satała G, Nitek W, Partyka A, Siwek A, Jankowska A, Wesołowska A, Kieć-Kononowicz K, Handzlik J.

Eur J Med Chem. 2018 Mar 10;147:102-114. doi: 10.1016/j.ejmech.2018.01.093. Epub 2018 Feb 1.

PMID:
29425815
37.

Anticonvulsant and reproductive toxicological studies of the imidazole-based histamine H3R antagonist 2-18 in mice.

Bastaki SM, Abdulrazzaq YM, Shafiullah M, Więcek M, Kieć-Kononowicz K, Sadek B.

Drug Des Devel Ther. 2018 Jan 19;12:179-194. doi: 10.2147/DDDT.S144730. eCollection 2018.

38.

Novel Multitarget-Directed Ligands Aiming at Symptoms and Causes of Alzheimer's Disease.

Więckowska A, Wichur T, Godyń J, Bucki A, Marcinkowska M, Siwek A, Więckowski K, Zaręba P, Knez D, Głuch-Lutwin M, Kazek G, Latacz G, Mika K, Kołaczkowski M, Korabecny J, Soukup O, Benkova M, Kieć-Kononowicz K, Gobec S, Malawska B.

ACS Chem Neurosci. 2018 May 16;9(5):1195-1214. doi: 10.1021/acschemneuro.8b00024. Epub 2018 Feb 13.

PMID:
29384656
39.

Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017).

Łażewska D, Kieć-Kononowicz K.

Expert Opin Ther Pat. 2018 Mar;28(3):175-196. doi: 10.1080/13543776.2018.1424135. Epub 2018 Jan 15. Review.

PMID:
29334795
40.

Selenazolinium Salts as "Small Molecule Catalysts" with High Potency against ESKAPE Bacterial Pathogens.

Witek K, Nasim MJ, Bischoff M, Gaupp R, Arsenyan P, Vasiljeva J, Marć MA, Olejarz A, Latacz G, Kieć-Kononowicz K, Handzlik J, Jacob C.

Molecules. 2017 Dec 8;22(12). pii: E2174. doi: 10.3390/molecules22122174.

41.

Histamine H3 Receptor Ligands in the Group of (Homo)piperazine Derivatives.

Szczepanska K, Kuder K, Kiec-Kononowicz K.

Curr Med Chem. 2018;25(14):1609-1626. doi: 10.2174/0929867325666171123203550. Review.

PMID:
29173145
42.

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

Jastrzębska-Więsek M, Siwek A, Partyka A, Kołaczkowski M, Walczak M, Smolik M, Latacz G, Kieć-Kononowicz K, Wesołowska A.

Naunyn Schmiedebergs Arch Pharmacol. 2018 Jan;391(1):37-49. doi: 10.1007/s00210-017-1431-y. Epub 2017 Oct 27.

43.

The Histamine H3 Receptor Antagonist E159 Reverses Memory Deficits Induced by Dizocilpine in Passive Avoidance and Novel Object Recognition Paradigm in Rats.

Alachkar A, Łażewska D, Kieć-Kononowicz K, Sadek B.

Front Pharmacol. 2017 Oct 12;8:709. doi: 10.3389/fphar.2017.00709. eCollection 2017.

44.

In Vitro Effects of Bromoalkyl Phenytoin Derivatives on Regulated Death, Cell Cycle and Ultrastructure of Leukemia Cells.

Śladowska K, Opydo-Chanek M, Król T, Trybus W, Trybus E, Kopacz-Bednarska A, Handzlik J, Kieć-Kononowicz K, Mazur L.

Anticancer Res. 2017 Nov;37(11):6373-6380.

PMID:
29061822
45.

Multifunctional Hybrid Compounds Derived from 2-(2,5-Dioxopyrrolidin-1-yl)-3-methoxypropanamides with Anticonvulsant and Antinociceptive Properties.

Abram M, Zagaja M, Mogilski S, Andres-Mach M, Latacz G, Baś S, Łuszczki JJ, Kieć-Kononowicz K, Kamiński K.

J Med Chem. 2017 Oct 26;60(20):8565-8579. doi: 10.1021/acs.jmedchem.7b01114. Epub 2017 Oct 4.

PMID:
28934547
46.

In the search for a lead structure among series of potent and selective hydantoin 5-HT7 R agents: The drug-likeness in vitro study.

Latacz G, Lubelska A, Jastrzębska-Więsek M, Partyka A, Sobiło A, Olejarz A, Kucwaj-Brysz K, Satała G, Bojarski AJ, Wesołowska A, Kieć-Kononowicz K, Handzlik J.

Chem Biol Drug Des. 2017 Dec;90(6):1295-1306. doi: 10.1111/cbdd.13106. Epub 2017 Oct 3.

PMID:
28886235
47.

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

Łażewska D, Kaleta M, Schwed JS, Karcz T, Mogilski S, Latacz G, Olejarz A, Siwek A, Kubacka M, Lubelska A, Honkisz E, Handzlik J, Filipek B, Stark H, Kieć-Kononowicz K.

Bioorg Med Chem. 2017 Oct 15;25(20):5341-5354. doi: 10.1016/j.bmc.2017.07.058. Epub 2017 Jul 29.

PMID:
28797771
48.

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

Szymańska E, Nielsen B, Johansen TN, Cuñado Moral AM, Pickering DS, Szczepańska K, Mickowska A, Kieć-Kononowicz K.

Eur J Med Chem. 2017 Sep 29;138:874-883. doi: 10.1016/j.ejmech.2017.07.007. Epub 2017 Jul 8.

PMID:
28738307
49.

In vitro cytotoxic activity evaluation of phenytoin derivatives against human leukemia cells.

Śladowska K, Handzlik J, Kieć-Kononowicz K, Mazur L.

Indian J Exp Biol. 2016 Sep;54(9):553-9.

PMID:
28699720
50.

Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands.

Szymańska E, Chałupnik P, Johansen TN, Nielsen B, Cuñado Moral AM, Pickering DS, Więckowska A, Kieć-Kononowicz K.

Chem Biol Drug Des. 2017 Dec;90(6):1271-1281. doi: 10.1111/cbdd.13048. Epub 2017 Jul 18.

PMID:
28636281

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