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Publications in the selection

32 hits

Bibliografisk träff 2024-02-23

Discovery of Novel Steroid-Based Histamine H3 Receptor Antagonists/Inverse Agonists.

Ledneczki I, Tapolcsányi P, Gábor E, Éles J, Barabás J, Béni Z, Varga B, Balázs O, Román V, Fodor L, Szikra J, Vastag M, Lévay G, Schmidt É, Lendvai B, Greiner I, Kiss B, Némethy Z, Mahó S.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c02117

Bibliografisk träff 2024-01-08

First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT6 Agents with a Beneficial Neuroprotective Profile against Alzheimer's Disease.

Pyka P, Haberek W, Więcek M, Szymanska E, Ali W, Cios A, Jastrzębska-Więsek M, Satała G, Podlewska S, Di Giacomo S, Di Sotto A, Garbo S, Karcz T, Lambona C, Marocco F, Latacz G, Sudoł-Tałaj S, Mordyl B, Głuch-Lutwin M, Siwek A, Czarnota-Łydka K, Gogola D, Olejarz-Maciej A, Wilczyńska-Zawal N, Honkisz-Orzechowska E, Starek M, Dąbrowska M, Kucwaj-Brysz K, Fioravanti R, Nasim MJ, Hittinger M, Partyka A, Wesołowska A, Battistelli C, Zwergel C, Handzlik J.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.3c02148

Bibliografisk träff 2023-10-17

Discovery of a Tritiated Radioligand with High Affinity and Selectivity for the Histamine H3 Receptor.

Mönnich D, Nagl M, Forster L, Rosier N, Igel P, Pockes S.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.3c00413

Bibliografisk träff 2023-07-19

A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.

Sutherland JJ, Yonchev D, Fekete A, Urban L.

Nat Commun · research support, non-u.s. gov't; research-article; journal article · DOI 10.1038/s41467-023-40064-9

Bibliografisk träff 2023-07-07

Dual Piperidine-Based Histamine H3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.

Szczepańska K, Karcz T, Dichiara M, Mogilski S, Kalinowska-Tłuścik J, Pilarski B, Leniak A, Pietruś W, Podlewska S, Popiołek-Barczyk K, Humphrys LJ, Ruiz-Cantero MC, Reiner-Link D, Leitzbach L, Łażewska D, Pockes S, Górka M, Zmysłowski A, Calmels T, Cobos EJ, Marrazzo A, Stark H, Bojarski AJ, Amata E, Kieć-Kononowicz K.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.3c00430

Bibliografisk träff 2022-12-16

Multitargeting approaches to cognitive impairment: Synthesis of aryl-alkylpiperazines and assessment at cholinesterases, histamine H3 and dopamine D3 receptors.

Aranha CMSQ, Reiner-Link D, Leitzbach LR, Lopes FB, Stark H, Fernandes JPS.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2022.117132

Bibliografisk träff 2022-09-09

A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.

Gu J, Wu Q, Zhang Q, You Q, Wang L.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2022.114742

Bibliografisk träff 2021-10-17

Histamine H3 receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation.

Falkenstein M, Reiner-Link D, Zivkovic A, Gering I, Willbold D, Stark H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2021.116462

Bibliografisk träff 2021-07-26

A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H3 Receptor.

Rosier N, Grätz L, Schihada H, Möller J, Işbilir A, Humphrys LJ, Nagl M, Seibel U, Lohse MJ, Pockes S.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c01089

Bibliografisk träff 2021-05-18

Designing Out PXR Activity on Drug Discovery Projects: A Review of Structure-Based Methods, Empirical and Computational Approaches.

Hall A, Chanteux H, Ménochet K, Ledecq M, Schulze MED.

J Med Chem · review; journal article · DOI 10.1021/acs.jmedchem.0c02245

Bibliografisk träff 2020-11-24

Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent.

Szczepańska K, Pockes S, Podlewska S, Höring C, Mika K, Latacz G, Bednarski M, Siwek A, Karcz T, Nagl M, Bresinsky M, Mönnich D, Seibel U, Kuder KJ, Kotańska M, Stark H, Elz S, Kieć-Kononowicz K.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.113041

Bibliografisk träff 2020-08-21

Rational design of new multitarget histamine H3 receptor ligands as potential candidates for treatment of Alzheimer's disease.

Łażewska D, Bajda M, Kaleta M, Zaręba P, Doroz-Płonka A, Siwek A, Alachkar A, Mogilski S, Saad A, Kuder K, Olejarz-Maciej A, Godyń J, Stary D, Sudoł S, Więcek M, Latacz G, Walczak M, Handzlik J, Sadek B, Malawska B, Kieć-Kononowicz K.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112743

Bibliografisk träff 2020-07-29

New drug approvals for 2019: Synthesis and clinical applications.

Yuan S, Yu B, Liu HM.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2020.112667

Bibliografisk träff 2020-02-14

Novel pyrrolidinone derivative lacks claimed histamine H3 receptor stimulation in receptor binding and functional studies.

Reiner D, Zivkovic A, Labeeuw O, Krief S, Capet M, Stark H.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112150

Bibliografisk träff 2019-10-17

Search for new multi-target compounds against Alzheimer's disease among histamine H3 receptor ligands.

Bajda M, Łażewska D, Godyń J, Zaręba P, Kuder K, Hagenow S, Łątka K, Stawarska E, Stark H, Kieć-Kononowicz K, Malawska B.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.111785

Bibliografisk träff 2019-07-31

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.

Vanda D, Zajdel P, Soural M.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2019.111569

Bibliografisk träff 2019-06-24

Sleep modulating agents.

Choi Y, Raymer BK.

Bioorg Med Chem Lett · review; journal article · DOI 10.1016/j.bmcl.2019.06.043

Bibliografisk träff 2018-04-25

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 · journal article · DOI 10.1016/j.ejmech.2018.04.043

Bibliografisk träff 2018-04-11

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 · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2018.04.023

Bibliografisk träff 2017-09-01

Discovery of novel steroidal histamine H3 receptor antagonists/inverse agonists.

Ledneczki I, Tapolcsányi P, Gábor E, Éles J, Greiner I, Schmidt É, Némethy Z, Kedves RS, Balázs O, Román V, Lévay G, Mahó S.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2017.08.060

Bibliografisk träff 2017-07-29

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 · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2017.07.058

Bibliografisk träff 2017-03-21

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

Kuder KJ, Łażewska D, Kaleta M, Latacz G, Kottke T, Olejarz A, Karcz T, Fruziński A, Szczepańska K, Karolak-Wojciechowska J, Stark H, Kieć-Kononowicz K.

Bioorg Med Chem · research support, non-u.s. gov't; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2017.03.031

Bibliografisk träff 2014-09-06

Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.

Lipani L, Odadzic D, Weizel L, Schwed JS, Sadek B, Stark H.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2014.09.011

Bibliografisk träff 2014-03-06

Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.

Sadek B, Schwed JS, Subramanian D, Weizel L, Walter M, Adem A, Stark H.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2014.03.014

Bibliografisk träff 2010-08-01

Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.

Walter M, Isensee K, Kottke T, Ligneau X, Camelin JC, Schwartz JC, Stark H.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2010.07.109

Bibliografisk träff 2010-08-01

Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.

Walter M, von Coburg Y, Isensee K, Sander K, Ligneau X, Camelin JC, Schwartz JC, Stark H.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2010.07.098

Bibliografisk träff 2009-07-01

5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.

Pierson PD, Fettes A, Freichel C, Gatti-McArthur S, Hertel C, Huwyler J, Mohr P, Nakagawa T, Nettekoven M, Plancher JM, Raab S, Richter H, Roche O, Rodríguez Sarmiento RM, Schmitt M, Schuler F, Takahashi T, Taylor S, Ullmer C, Wiegand R.

J Med Chem · journal article · DOI 10.1021/jm900409x

Bibliografisk träff 2009-06-16

Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.

Swanson DM, Shah CR, Lord B, Morton K, Dvorak LK, Mazur C, Apodaca R, Xiao W, Boggs JD, Feinstein M, Wilson SJ, Barbier AJ, Bonaventure P, Lovenberg TW, Carruthers NI.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2009.06.007

Bibliografisk träff 2009-03-14

Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.

Łazewska D, Kuder K, Ligneau X, Camelin JC, Schunack W, Stark H, Kieć-Kononowicz K.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2009.03.014

Bibliografisk träff 2009-03-03

Fluorinated non-imidazole histamine H3 receptor antagonists.

Isensee K, Amon M, Garlapati A, Ligneau X, Camelin JC, Capet M, Schwartz JC, Stark H.

Bioorg Med Chem Lett · comparative study; research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2009.02.110

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Publications in the selection

Discovery of Novel Steroid-Based Histamine H<sub>3</sub> Receptor Antagonists/Inverse Agonists.

First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT<sub>6</sub> Agents with a Beneficial Neuroprotective Profile against Alzheimer's Disease.

Discovery of a Tritiated Radioligand with High Affinity and Selectivity for the Histamine H<sub>3</sub> Receptor.

A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.

Dual Piperidine-Based Histamine H<sub>3</sub> and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.

Multitargeting approaches to cognitive impairment: Synthesis of aryl-alkylpiperazines and assessment at cholinesterases, histamine H<sub>3</sub> and dopamine D<sub>3</sub> receptors.

A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.

Histamine H<sub>3</sub> receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation.

A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H<sub>3</sub> Receptor.

Designing Out PXR Activity on Drug Discovery Projects: A Review of Structure-Based Methods, Empirical and Computational Approaches.

Structural modifications in the distal, regulatory region of histamine H<sub>3</sub> receptor antagonists leading to the identification of a potent anti-obesity agent.

Rational design of new multitarget histamine H<sub>3</sub> receptor ligands as potential candidates for treatment of Alzheimer's disease.

New drug approvals for 2019: Synthesis and clinical applications.

Novel pyrrolidinone derivative lacks claimed histamine H<sub>3</sub> receptor stimulation in receptor binding and functional studies.

Search for new multi-target compounds against Alzheimer's disease among histamine H<sub>3</sub> receptor ligands.

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.

Sleep modulating agents.

Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H<sub>3</sub>R ligands.

Novel naphthyloxy derivatives - Potent histamine H<sub>3</sub> receptor ligands. Synthesis and pharmacological evaluation.

Discovery of novel steroidal histamine H<sub>3</sub> receptor antagonists/inverse agonists.

Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H<sub>3</sub> receptor ligands.

Synthesis and biological activity of novel tert-amylphenoxyalkyl (homo)piperidine derivatives as histamine H<sub>3</sub>R ligands.

Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.

Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.

Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.

Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.

5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.

Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.

Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.

Fluorinated non-imidazole histamine H3 receptor antagonists.