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Publikationer i urvalet

40 träffar

Bibliografisk träff 2024-06-14

Dual 5-HT6/SERT ligands for mitigating neuropsychiatric symptoms of dementia exerting neuroprotection against amyloid-β toxicity, memory preservation, and antidepressant-like properties.

Siwek A, Marcinkowska M, Głuch-Lutwin M, Mordyl B, Wolak M, Jastrzębska-Więsek M, Wilczyńska-Zawal N, Wyska E, Szafrańska K, Karcz T, Ostrowska O, Bucki A, Kołaczkowski M.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2024.116601

Bibliografisk träff 2024-01-13

Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel.

Zhang SM, Paulin CBJ, Shu H, Yagüe-Capilla M, Michel M, Marttila P, Ortis F, Bwanika HC, Dirks C, Venkatram RP, Wiita E, Jemth AS, Almlöf I, Loseva O, Hormann FM, Koolmeister T, Linde E, Lee S, Llona-Minguez S, Haraldsson M, Axelsson H, Strömberg K, Homan EJ, Scobie M, Lundbäck T, Helleday T, Rudd SG.

iScience · research-article; journal article · DOI 10.1016/j.isci.2024.108907

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 2022-12-29

Hybrid molecules combining GABA-A and serotonin 5-HT6 receptors activity designed to tackle neuroinflammation associated with depression.

Marcinkowska M, Mordyl B, Fajkis-Zajaczkowska N, Siwek A, Karcz T, Gawalska A, Bucki A, Żmudzki P, Partyka A, Jastrzębska-Więsek M, Pomierny B, Walczak M, Smolik M, Pytka K, Mika K, Kotańska M, Kolaczkowski M.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.115071

Bibliografisk träff 2022-03-29

Inhibition of the drug efflux activity of Ptch1 as a promising strategy to overcome chemotherapy resistance in cancer cells.

Kovachka S, Malloci G, Simsir M, Ruggerone P, Azoulay S, Mus-Veteau I.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2022.114306

Bibliografisk träff 2021-08-27

Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT6R antagonists with β-amyloid anti-aggregation properties.

Wichur T, Godyń J, Góral I, Latacz G, Bucki A, Siwek A, Głuch-Lutwin M, Mordyl B, Śniecikowska J, Walczak M, Knez D, Jukič M, Sałat K, Gobec S, Kołaczkowski M, Malawska B, Brazzolotto X, Więckowska A.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113792

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 2021-08-19

Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT6 receptor with anti-aggregation properties against amyloid-beta and tau.

Wichur T, Pasieka A, Godyń J, Panek D, Góral I, Latacz G, Honkisz-Orzechowska E, Bucki A, Siwek A, Głuch-Lutwin M, Knez D, Brazzolotto X, Gobec S, Kołaczkowski M, Sabate R, Malawska B, Więckowska A.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113783

Bibliografisk träff 2020-09-01

Pharmacological Analysis of the Anti-inflammatory and Antiallodynic Effects of Zinagrandinolide E from Zinnia grandiflora in Mice.

Reyes-Pérez VI, Granados-Soto V, Rangel-Grimaldo M, Déciga-Campos M, Mata R.

J Nat Prod · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jnatprod.0c00793

Bibliografisk träff 2020-08-20

Isoquinolinone derivatives as potent CNS multi-receptor D2/5-HT1A/5-HT2A/5-HT6/5-HT7 agents: Synthesis and pharmacological evaluation.

Jin J, Zhang K, Dou F, Hao C, Zhang Y, Cao X, Gao L, Xiong J, Liu X, Liu BF, Zhang G, Chen Y.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112709

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 2019-09-16

Structure-activity relationships of serotonin 5-HT7 receptors ligands: A review.

Thirumaran SL, Lepailleur A, Rochais C.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2019.111705

Bibliografisk träff 2019-09-15

Synthesis and antidepressant effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7.

Gu ZS, Wang WT, Qian H, Zhou AN, Sun HB, Zhang QW, Li JQ.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2019.126703

Bibliografisk träff 2019-07-30

Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.

Czopek A, Bucki A, Kołaczkowski M, Zagórska A, Drop M, Pawłowski M, Siwek A, Głuch-Lutwin M, Pękala E, Chrzanowska A, Struga M, Partyka A, Wesołowska A.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2019.07.046

Bibliografisk träff 2019-07-12

Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT1A receptor ligands.

Ślifirski G, Król M, Kleps J, Podsadni P, Belka M, Bączek T, Siwek A, Stachowicz K, Szewczyk B, Nowak G, Bojarski A, Kozioł AE, Turło J, Herold F.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.07.027

Bibliografisk träff 2019-06-03

Mapping human microbiome drug metabolism by gut bacteria and their genes.

Zimmermann M, Zimmermann-Kogadeeva M, Wegmann R, Goodman AL.

Nature · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1038/s41586-019-1291-3

Bibliografisk träff 2018-04-25

Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.

Pańczyk K, Pytka K, Jakubczyk M, Rapacz A, Sałat K, Furgała A, Siwek A, Głuch-Lutwin M, Gryboś A, Słoczyńska K, Pękala E, Żmudzki P, Bucki A, Kołaczkowski M, Żelaszczyk D, Marona H, Waszkielewicz AM.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2018.04.059

Bibliografisk träff 2018-01-03

Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.

Zajdel P, Kos T, Marciniec K, Satała G, Canale V, Kamiński K, Hołuj M, Lenda T, Koralewski R, Bednarski M, Nowiński L, Wójcikowski J, Daniel WA, Nikiforuk A, Nalepa I, Chmielarz P, Kuśmierczyk J, Bojarski AJ, Popik P.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.01.002

Bibliografisk träff 2017-08-18

Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.

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

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.7b00839

Bibliografisk träff 2016-09-15

Synthesis and activity of newly designed aroxyalkyl or aroxyethoxyethyl derivatives of piperazine on the cardiovascular and the central nervous systems.

Waszkielewicz AM, Kubacka M, Pańczyk K, Mogilski S, Siwek A, Głuch-Lutwin M, Gryboś A, Filipek B.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2016.09.037

Bibliografisk träff 2016-03-11

Synthesis of azepino[4,5-b]indol-4-ones via MCR/free radical cyclization and in vitro-in silico studies as 5-Ht₆R ligands.

Rentería-Gómez A, Islas-Jácome A, Díaz-Cervantes E, Villaseñor-Granados T, Robles J, Gámez-Montaño R.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2016.03.036

Bibliografisk träff 2016-02-09

Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.

Kucwaj-Brysz K, Warszycki D, Podlewska S, Witek J, Witek K, González Izquierdo A, Satała G, Loza MI, Lubelska A, Latacz G, Bojarski AJ, Castro M, Kieć-Kononowicz K, Handzlik J.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2016.02.024

Bibliografisk träff 2015-05-01

Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.

Zagórska A, Kołaczkowski M, Bucki A, Siwek A, Kazek G, Satała G, Bojarski AJ, Partyka A, Wesołowska A, Pawłowski M.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2015.04.046

Bibliografisk träff 2015-02-13

In vitro and in silico evaluation of twelve newly-synthesized 1-acetamide-5-methoxy-2-oxindoles as 5-Ht₇ receptor ligands.

Díaz-Cervantes E, Islas-Jácome A, Rentería-Gómez A, Robles J, Gámez-Montaño R.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2015.02.008

Bibliografisk träff 2014-12-24

Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.

Kołaczkowski M, Marcinkowska M, Bucki A, Śniecikowska J, Pawłowski M, Kazek G, Siwek A, Jastrzębska-Więsek M, Partyka A, Wasik A, Wesołowska A, Mierzejewski P, Bienkowski P.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2014.12.045

Bibliografisk träff 2014-07-04

Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?

Tschammer N.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2014.06.082

Bibliografisk träff 2014-05-23

Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.

Kołaczkowski M, Marcinkowska M, Bucki A, Pawłowski M, Mitka K, Jaśkowska J, Kowalski P, Kazek G, Siwek A, Wasik A, Wesołowska A, Mierzejewski P, Bienkowski P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm401895u

Bibliografisk träff 2013-02-27

Novel pyrimidoazepine analogs as serotonin 5-HT(2A) and 5-HT(2C) receptor ligands for the treatment of obesity.

Yang HY, Tae J, Seo YW, Kim YJ, Im HY, Choi GD, Cho H, Park WK, Kwon OS, Cho YS, Ko M, Jang H, Lee J, Choi K, Kim CH, Lee J, Pae AN.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2013.02.020

Bibliografisk träff 2012-08-04

The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists.

Zajdel P, Kurczab R, Grychowska K, Satała G, Pawłowski M, Bojarski AJ.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2012.07.043

Bibliografisk träff 2011-07-02

Identification of novel allosteric modulators for the G-protein coupled US28 receptor of human cytomegalovirus.

Kralj A, Wetzel A, Mahmoudian S, Stamminger T, Tschammer N, Heinrich MR.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2011.06.120

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Publikationer i urvalet

Dual 5-HT<sub>6</sub>/SERT ligands for mitigating neuropsychiatric symptoms of dementia exerting neuroprotection against amyloid-β toxicity, memory preservation, and antidepressant-like properties.

Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel.

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

Hybrid molecules combining GABA-A and serotonin 5-HT<sub>6</sub> receptors activity designed to tackle neuroinflammation associated with depression.

Inhibition of the drug efflux activity of Ptch1 as a promising strategy to overcome chemotherapy resistance in cancer cells.

Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT<sub>6</sub>R antagonists with β-amyloid anti-aggregation properties.

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

Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT<sub>6</sub> receptor with anti-aggregation properties against amyloid-beta and tau.

Pharmacological Analysis of the Anti-inflammatory and Antiallodynic Effects of Zinagrandinolide E from <i>Zinnia grandiflora</i> in Mice.

Isoquinolinone derivatives as potent CNS multi-receptor D<sub>2</sub>/5-HT<sub>1A</sub>/5-HT<sub>2A</sub>/5-HT<sub>6</sub>/5-HT<sub>7</sub> agents: Synthesis and pharmacological evaluation.

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

Structure-activity relationships of serotonin 5-HT<sub>7</sub> receptors ligands: A review.

Synthesis and antidepressant effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT<sub>1A</sub>/5-HT<sub>7</sub>.

Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.

Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT<sub>1A</sub> receptor ligands.

Mapping human microbiome drug metabolism by gut bacteria and their genes.

Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.

Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.

Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.

Synthesis and activity of newly designed aroxyalkyl or aroxyethoxyethyl derivatives of piperazine on the cardiovascular and the central nervous systems.

Synthesis of azepino[4,5-b]indol-4-ones via MCR/free radical cyclization and in vitro-in silico studies as 5-Ht₆R ligands.

Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.

Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.

In vitro and in silico evaluation of twelve newly-synthesized 1-acetamide-5-methoxy-2-oxindoles as 5-Ht₇ receptor ligands.

Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.

Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?

Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.

Novel pyrimidoazepine analogs as serotonin 5-HT(2A) and 5-HT(2C) receptor ligands for the treatment of obesity.

The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists.

Identification of novel allosteric modulators for the G-protein coupled US28 receptor of human cytomegalovirus.