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Publikationer i urvalet

12 träffar

Bibliografisk träff 2023-03-21

Novel thienocycloalkylpyridazinones as useful scaffolds for acetylcholinesterase inhibition and serotonin 5-HT6 receptor interaction.

Asproni B, Catto M, Loriga G, Murineddu G, Corona P, Purgatorio R, Cichero E, Fossa P, Scarano N, Martínez AL, Brea J, Pinna GA.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2023.117256

Bibliografisk träff 2022-07-29

Novel difluoromethylated 1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole derivatives as potent 5-HT6 receptor antagonist with AMDE-improving properties: Design, synthesis, and biological evaluation.

Yi C, Chen K, Liang H, Wang Z, Wang T, Li K, Yu J, Sun J, Jin C.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2022.116950

Bibliografisk träff 2022-07-01

Novel difluoromethyl-containing 1-((4-methoxy-3-(piperazin-1-yl)phenyl)sulfonyl)-1H-indole scaffold as potent 5-HT6R antagonists: Design, synthesis, biological evaluation, and early in vivo cognition-enhancing studies.

Yi C, Xue Y, Chen K, Wang T, Yu J, Wang Z, Jin C.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2022.116917

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 2020-12-03

Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT6 receptor antagonist with therapeutic interest in Alzheimer's disease.

Toublet FX, Lalut J, Hatat B, Lecoutey C, Davis A, Since M, Corvaisier S, Freret T, Sopková-de Oliveira Santos J, Claeysen S, Boulouard M, Dallemagne P, Rochais C.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.113059

Bibliografisk träff 2019-11-07

Virtual screening-driven discovery of dual 5-HT6/5-HT2A receptor ligands with pro-cognitive properties.

Staroń J, Kurczab R, Warszycki D, Satała G, Krawczyk M, Bugno R, Lenda T, Popik P, Hogendorf AS, Hogendorf A, Dubiel K, Matłoka M, Moszczyński-Pętkowski R, Pieczykolan J, Wieczorek M, Zajdel P, Bojarski AJ.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.111857

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 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

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Publikationer i urvalet

Novel thienocycloalkylpyridazinones as useful scaffolds for acetylcholinesterase inhibition and serotonin 5-HT<sub>6</sub> receptor interaction.

Novel difluoromethylated 1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole derivatives as potent 5-HT<sub>6</sub> receptor antagonist with AMDE-improving properties: Design, synthesis, and biological evaluation.

Novel difluoromethyl-containing 1-((4-methoxy-3-(piperazin-1-yl)phenyl)sulfonyl)-1H-indole scaffold as potent 5-HT<sub>6</sub>R antagonists: Design, synthesis, biological evaluation, and early in vivo cognition-enhancing studies.

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.

Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT<sub>6</sub> receptor antagonist with therapeutic interest in Alzheimer's disease.

Virtual screening-driven discovery of dual 5-HT<sub>6</sub>/5-HT<sub>2A</sub> receptor ligands with pro-cognitive properties.

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

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.