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Publikationer i urvalet

22 träffar

Bibliografisk träff 2024-06-21

5-HT6 receptor neutral antagonists protect astrocytes: A lesson from 2-phenylpyrrole derivatives.

Drop M, Koczurkiewicz-Adamczyk P, Bento O, Pietruś W, Satała G, Blicharz-Futera K, Canale V, Grychowska K, Bantreil X, Pękala E, Kurczab R, Bojarski AJ, Chaumont-Dubel S, Marin P, Lamaty F, Zajdel P.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2024.116615

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 2023-10-06

5-HT6 receptor antagonists. Design, synthesis, and structure-activity relationship of substituted 2-(1-methyl-4-piperazinyl)pyridines.

Gałęzowski M, Fabritius CH, Pesonen U, Salo H, Olszak-Płachta M, Czerwińska K, Adamczyk J, Król M, Prusis P, Sieprawska-Lupa M, Mikulski M, Kuokkanen K, Obuchowicz R, Korjamo T, Jalava N, Nikiforuk A, Nowak M.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2023.129497

Bibliografisk träff 2023-10-05

Superiority of the Triple-Acting 5-HT6R/5-HT3R Antagonist and MAO-B Reversible Inhibitor PZ-1922 over 5-HT6R Antagonist Intepirdine in Alleviation of Cognitive Deficits in Rats.

Grychowska K, López-Sánchez U, Vitalis M, Canet G, Satała G, Olejarz-Maciej A, Gołębiowska J, Kurczab R, Pietruś W, Kubacka M, Moreau C, Walczak M, Blicharz-Futera K, Bento O, Bantreil X, Subra G, Bojarski AJ, Lamaty F, Becamel C, Zussy C, Chaumont-Dubel S, Popik P, Nury H, Marin P, Givalois L, Zajdel P.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.3c01482

Bibliografisk träff 2021-09-01

Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT3 and 5-HT6 Receptor Antagonist with Antipsychotic and Procognitive Properties.

Zajdel P, Grychowska K, Mogilski S, Kurczab R, Satała G, Bugno R, Kos T, Gołębiowska J, Malikowska-Racia N, Nikiforuk A, Chaumont-Dubel S, Bantreil X, Pawłowski M, Martinez J, Subra G, Lamaty F, Marin P, Bojarski AJ, Popik P.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.1c00224

Bibliografisk träff 2021-08-26

Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.

Marcinkowska M, Bucki A, Sniecikowska J, Zagórska A, Fajkis-Zajączkowska N, Siwek A, Gluch-Lutwin M, Żmudzki P, Jastrzebska-Wiesek M, Partyka A, Wesołowska A, Abram M, Przejczowska-Pomierny K, Cios A, Wyska E, Mika K, Kotańska M, Mierzejewski P, Kolaczkowski M.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.1c00497

Bibliografisk träff 2021-07-23

Chemical update on the potential for serotonin 5-HT6 and 5-HT7 receptor agents in the treatment of Alzheimer's disease.

Kucwaj-Brysz K, Baltrukevich H, Czarnota K, Handzlik J.

Bioorg Med Chem Lett · research support, non-u.s. gov't; review; journal article · DOI 10.1016/j.bmcl.2021.128275

Bibliografisk träff 2021-01-13

Imidazopyridine-Based 5-HT6 Receptor Neutral Antagonists: Impact of N1-Benzyl and N1-Phenylsulfonyl Fragments on Different Receptor Conformational States.

Vanda D, Canale V, Chaumont-Dubel S, Kurczab R, Satała G, Koczurkiewicz-Adamczyk P, Krawczyk M, Pietruś W, Blicharz K, Pękala E, Bojarski AJ, Popik P, Marin P, Soural M, Zajdel P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.0c02009

Bibliografisk träff 2020-08-22

A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties.

Canale V, Grychowska K, Kurczab R, Ryng M, Keeri AR, Satała G, Olejarz-Maciej A, Koczurkiewicz P, Drop M, Blicharz K, Piska K, Pękala E, Janiszewska P, Krawczyk M, Walczak M, Chaumont-Dubel S, Bojarski AJ, Marin P, Popik P, Zajdel P.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112765

Bibliografisk träff 2020-02-18

Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).

Bucki A, Marcinkowska M, Śniecikowska J, Zagórska A, Jamrozik M, Pawłowski M, Głuch-Lutwin M, Siwek A, Jakubczyk M, Pytka K, Jastrzębska-Więsek M, Partyka A, Wesołowska A, Mierzejewski P, Kołaczkowski M.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112149

Bibliografisk träff 2019-06-10

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 · journal article · DOI 10.1016/j.ejmech.2019.06.022

Bibliografisk träff 2019-06-05

2-Aminoimidazole-based antagonists of the 5-HT6 receptor - A new concept in aminergic GPCR ligand design.

Hogendorf AS, Hogendorf A, Kurczab R, Kalinowska-Tłuścik J, Popik P, Nikiforuk A, Krawczyk M, Satała G, Lenda T, Knutelska J, Bugno R, Staroń J, Pietruś W, Matłoka M, Dubiel K, Moszczyński-Pętkowski R, Pieczykolan J, Wieczorek M, Pilarski B, Zajdel P, Bojarski AJ.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.06.001

Bibliografisk träff 2018-05-23

Pyrroloquinoline scaffold-based 5-HT6R ligands: Synthesis, quantum chemical and molecular dynamic studies, and influence of nitrogen atom position in the scaffold on affinity.

Grychowska K, Kurczab R, Śliwa P, Satała G, Dubiel K, Matłoka M, Moszczyński-Pętkowski R, Pieczykolan J, Bojarski AJ, Zajdel P.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2018.05.033

Bibliografisk träff 2017-12-16

Novel non-sulfonamide 5-HT6 receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties.

Vanda D, Soural M, Canale V, Chaumont-Dubel S, Satała G, Kos T, Funk P, Fülöpová V, Lemrová B, Koczurkiewicz P, Pękala E, Bojarski AJ, Popik P, Marin P, Zajdel P.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2017.12.053

Bibliografisk träff 2017-02-17

Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT6) Receptor Antagonist for Potential Treatment of Alzheimer's Disease.

Nirogi R, Shinde A, Kambhampati RS, Mohammed AR, Saraf SK, Badange RK, Bandyala TR, Bhatta V, Bojja K, Reballi V, Subramanian R, Benade V, Palacharla RC, Bhyrapuneni G, Jayarajan P, Goyal V, Jasti V.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.6b01662

Bibliografisk träff 2016-04-07

N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.

Zajdel P, Marciniec K, Satała G, Canale V, Kos T, Partyka A, Jastrzębska-Więsek M, Wesołowska A, Basińska-Ziobroń A, Wójcikowski J, Daniel WA, Bojarski AJ, Popik P, Popik P.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.6b00056

Bibliografisk träff 2014-06-18

Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.

Krogsgaard-Larsen N, Jensen AA, Schrøder TJ, Christoffersen CT, Kehler J.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm5003759

Bibliografisk träff 2014-06-03

Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease.

Benhamú B, Martín-Fontecha M, Vázquez-Villa H, Pardo L, López-Rodríguez ML.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/jm5003952

Bibliografisk träff 2013-06-01

Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-НТ6 receptors.

Ivachtchenko A, Golovina E, Kadieva M, Mitkin O, Tkachenko S, Okun I.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2013.05.040

Bibliografisk träff 2011-12-13

Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test.

Tripathy R, McHugh RJ, Bacon ER, Salvino JM, Morton GC, Aimone LD, Huang Z, Mathiasen JR, DiCamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Qian J, Angeles TS, Connors T, Spais C, Holskin B, Duzic E, Schaffhauser H, Rossé GC.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2011.12.026

Bibliografisk träff 2010-07-01

(3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor.

Ivachtchenko AV, Dmitriev DE, Golovina ES, Kadieva MG, Koryakova AG, Kysil VM, Mitkin OD, Okun IM, Tkachenko SE, Vorobiev AA.

J Med Chem · journal article · DOI 10.1021/jm100350r

Bibliografisk träff 2009-05-03

Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands.

Liu KG, Lo JR, Comery TA, Zhang GM, Zhang JY, Kowal DM, Smith DL, Di L, Kerns EH, Schechter LE, Robichaud AJ.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2009.04.108

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Publikationer i urvalet

5-HT<sub>6</sub> receptor neutral antagonists protect astrocytes: A lesson from 2-phenylpyrrole derivatives.

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

5-HT<sub>6</sub> receptor antagonists. Design, synthesis, and structure-activity relationship of substituted 2-(1-methyl-4-piperazinyl)pyridines.

Superiority of the Triple-Acting 5-HT<sub>6</sub>R/5-HT<sub>3</sub>R Antagonist and MAO-B Reversible Inhibitor <b>PZ-1922</b> over 5-HT<sub>6</sub>R Antagonist Intepirdine in Alleviation of Cognitive Deficits in Rats.

Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT<sub>3</sub> and 5-HT<sub>6</sub> Receptor Antagonist with Antipsychotic and Procognitive Properties.

Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.

Chemical update on the potential for serotonin 5-HT<sub>6</sub> and 5-HT<sub>7</sub> receptor agents in the treatment of Alzheimer's disease.

Imidazopyridine-Based 5-HT<sub>6</sub> Receptor Neutral Antagonists: Impact of <i>N</i><sup>1</sup>-Benzyl and <i>N</i><sup>1</sup>-Phenylsulfonyl Fragments on Different Receptor Conformational States.

A dual-acting 5-HT<sub>6</sub> receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties.

Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).

Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT<sub>6</sub>.

2-Aminoimidazole-based antagonists of the 5-HT<sub>6</sub> receptor - A new concept in aminergic GPCR ligand design.

Pyrroloquinoline scaffold-based 5-HT<sub>6</sub>R ligands: Synthesis, quantum chemical and molecular dynamic studies, and influence of nitrogen atom position in the scaffold on affinity.

Novel non-sulfonamide 5-HT<sub>6</sub> receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties.

Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT<sub>6</sub>) Receptor Antagonist for Potential Treatment of Alzheimer's Disease.

N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.

Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.

Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease.

Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-НТ6 receptors.

Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test.

(3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor.

Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands.