Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Zsolt Szombathelyi"'
Autor:
Attila Sándor Halász, Amrita Ágnes Bobok, Zoltán Szakács, István Greiner, Zoltán Orgován, Mónika Vastag, Sándor Kolok, Zoltán Béni, Gábor Wágner, Mónika L. Mikó-Bakk, Zsolt Szombathelyi, Attila Bielik, Krisztina Gál, Katalin Nogradi, György M. Keserű, Ottilia Balázs, Katalin Saghy, János Kóti, György T. Balogh, Judit Laszy, Mikhail Krasavin, György Domány, Janos Galambos
Publikováno v:
Journal of Medicinal Chemistry. 60:2470-2484
Negative allosteric modulators (NAM) of metabotropic glutamate receptor 5 (mGluR5) have been implicated as a potential pharmacotherapy for a number of psychiatric diseases, including anxiety and depression. Most of the mGluR5 NAM clinical candidates
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e3dc984e3e83f573a4bc24f797febd2
https://doi.org/10.1021/acs.jmedchem.6b01858
https://doi.org/10.1021/acs.jmedchem.6b01858
Autor:
Áron Szigetvári, Mónika Vastag, Katalin Saghy, Zoltán Orgován, Zoltán Béni, Attila Bielik, István Greiner, Zsuzsanna Sánta, György Domány, Janos Galambos, Amrita Ágnes Bobok, Mikhail Krasavin, Zsolt Szombathelyi, János Kóti, Gábor Wágner, Mónika L. Mikó-Bakk, Krisztina Gál, György M. Keserű, Bela Kiss
Publikováno v:
European Journal of Medicinal Chemistry, 133, 240-254. Elsevier Masson SAS
Galambos, J, Bielik, A, Wágner, G, Domány, G, Kóti, J, Béni, Z, Szigetvári, Á, Sánta, Z, Orgován, Z, Bobok, A, Kiss, B, Mikó-Bakk, M L, Vastag, M, Sághy, K, Krasavin, M, Gál, K, Greiner, I, Szombathelyi, Z & Keserű, G M 2017, ' Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu 5 ) receptor negative allosteric modulators ', European Journal of Medicinal Chemistry, vol. 133, pp. 240-254 . https://doi.org/10.1016/j.ejmech.2017.03.071
Galambos, J, Bielik, A, Wágner, G, Domány, G, Kóti, J, Béni, Z, Szigetvári, Á, Sánta, Z, Orgován, Z, Bobok, A, Kiss, B, Mikó-Bakk, M L, Vastag, M, Sághy, K, Krasavin, M, Gál, K, Greiner, I, Szombathelyi, Z & Keserű, G M 2017, ' Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu 5 ) receptor negative allosteric modulators ', European Journal of Medicinal Chemistry, vol. 133, pp. 240-254 . https://doi.org/10.1016/j.ejmech.2017.03.071
Negative allosteric modulators of metabotropic glutamate receptor 5 (mGlu5) showed efficacy in a number of animal models of different CNS diseases including anxiety and depression. Virtually all of the compounds which reached the clinic belong to the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e982dd919be3bfceb66d1c088d5ac9e5
https://doi.org/10.1016/j.ejmech.2017.03.071
https://doi.org/10.1016/j.ejmech.2017.03.071
Autor:
Katalin Nógrádi, Gábor Wágner, György Domány, Amrita Bobok, Ildikó Magdó, Sándor Kolok, Mónika L. Mikó-Bakk, Mónika Vastag, Katalin Sághy, István Gyertyán, János Kóti, Krisztina Gál, Sándor Farkas, György M. Keserű, István Greiner, Zsolt Szombathelyi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1724-1729
An HTS campaign of our corporate compound library, and hit-to lead development resulted in thieno[2,3-b]pyridine derivative leads with mGluR5 negative allosteric modulator effects. During the lead optimization process, our objective was to improve af
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd62fc22399e4fa88fe813230edc0ffe
https://doi.org/10.1016/j.bmcl.2015.02.073
https://doi.org/10.1016/j.bmcl.2015.02.073
Autor:
János, Galambos, Attila, Bielik, Gábor, Wágner, György, Domány, János, Kóti, Zoltán, Béni, Áron, Szigetvári, Zsuzsanna, Sánta, Zoltán, Orgován, Amrita, Bobok, Béla, Kiss, Mónika L, Mikó-Bakk, Mónika, Vastag, Katalin, Sághy, Mikhail, Krasavin, Krisztina, Gál, István, Greiner, Zsolt, Szombathelyi, György M, Keserű
Publikováno v:
European journal of medicinal chemistry. 133
Negative allosteric modulators of metabotropic glutamate receptor 5 (mGlu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::aca93a6027a9c2b2d4f26d121afc3ef1
https://pubmed.ncbi.nlm.nih.gov/28390229
https://pubmed.ncbi.nlm.nih.gov/28390229
Autor:
Katalin Fónagy, Krisztina Gál, Sándor Farkas, György M. Keserű, Ildikó Magdó, Bela Kiss, Gábor Wágner, Katalin Nogradi, Zsolt Szombathelyi, Sándor Kolok, Viktor Háda, János Kóti, Amrita Ágnes Bobok, Istvan Gyertyan, István Greiner, György Domány
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3845-3849
An HTS campaign of our corporate compound library resulted in thieno[2,3-b]pyridines derivative hits with mGluR5 negative allosteric modulator effects. During the hit-to-lead development our objective was to improve affinity, and to keep the ligand e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e17c5b02fdae6f3e4eeebfbae763785
https://doi.org/10.1016/j.bmcl.2014.06.057
https://doi.org/10.1016/j.bmcl.2014.06.057
Autor:
Amrita Ágnes Bobok, György Domány, Zoltán Szakács, Krisztina Gál, Katalin Saghy, György M. Keserű, Katalin Nogradi, Zsolt Szombathelyi, Sándor Kolok, Janos Galambos, János Kóti, Zoltán Béni, István Greiner, Gábor Wágner, Mónika L. Mikó-Bakk, Mónika Vastag
Publikováno v:
Galambos, J, Domány, G, Nógrádi, K, Wágner, G, Keseru, G M, Bobok, A, Kolok, S, Mikó-Bakk, M L, Vastag, M, Sághy, K, Kóti, J, Szakács, Z, Béni, Z, Gál, K, Szombathelyi, Z & Greiner, I 2016, ' 4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors : From HTS hit to development candidate ', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 4, pp. 1249-1252 . https://doi.org/10.1016/j.bmcl.2016.01.024
Bioorganic and Medicinal Chemistry Letters, 26(4), 1249-1252. Elsevier Limited
Bioorganic and Medicinal Chemistry Letters, 26(4), 1249-1252. Elsevier Limited
High throughput screening of our corporate compound library followed by hit-to-lead development resulted in a 4-aryl-3-arylsulfonyl-quinoline derivative lead (2) with mGluR5 negative allosteric modulator activity. During the lead optimization process
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34b9293cfa61b23617d4ae5ab3c9f312
https://research.vu.nl/en/publications/90c75f64-ce57-4f0f-aa17-4c3a16a1765e
https://research.vu.nl/en/publications/90c75f64-ce57-4f0f-aa17-4c3a16a1765e
Autor:
Mária Zájer-Balázs, Károly Tihanyi, Katalin Saghy, Mónika Vastag, Katalin Nogradi, Istvan Vago, Bela Kiss, Margit Kapás, István Greiner, Larisza Gémesi, Zsolt Szombathelyi, György M. Keserű, Éva Ágai-Csongor, Janos Galambos, Eva Schmidt, Istvan Gyertyan, György Domány, Judit Laszy, Aniko Gere, István Laszlovszky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3437-3440
Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D3/D2 compound (1) led to a series of new piperazine derivatives having affinity to both dopamine D3 and D2 receptors. Severa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87b1e35c4f2a245e7be871e82a9552b3
https://doi.org/10.1016/j.bmcl.2012.03.104
https://doi.org/10.1016/j.bmcl.2012.03.104
Autor:
Zsolt Szombathelyi, István Likó, Norbert Solymosi, Erik Hrabovszky, Béla Molnár, Károly Tihanyi, Orsolya Galamb, Imre Kalló, Zsolt Liposits, Miklós Sárvári
Publikováno v:
Endocrinology. 151:1161-1176
Estradiol modulates a wide range of neural functions in the frontal cerebral cortex where subsets of neurons express estrogen receptor-α and -β. Through these receptors, estradiol contributes to the maintenance of normal operation of the frontal co
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ad2dd194f777ae43470b8777b684e62
https://doi.org/10.1210/en.2009-0911
https://doi.org/10.1210/en.2009-0911
Autor:
József Nagy, Sándor Kolok, Zsófia Bekes, Aniko Gere, Gyula Bugovics, András Boros, Zsolt Szombathelyi, Andrea Baki, Dalma Kurkó, Györgyi Ignácz-Szendrei
Publikováno v:
Neurochemistry International. 55:467-475
Adrenergic alpha(1), alpha(2) and beta receptors are members of the G-protein-coupled receptor families (GPCRs) mediating physiological responses to adrenaline (epinephrine) and noradrenaline (norepinephrine). Since GPCRs are major targets for potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be5483a1bf4e94001593b00e7cf4bfbf
https://doi.org/10.1016/j.neuint.2009.04.015
https://doi.org/10.1016/j.neuint.2009.04.015
Autor:
Paul G.M. Luiten, Károly Tihanyi, Jan N. Keijser, Csaba Nyakas, Zsolt Szombathelyi, Robert Szabo, Klara Felszeghy
Publikováno v:
CNS Neuroscience & Therapeutics, 15(2), 89-99. Wiley
Vinpocetine (ethyl-apovincaminate, Cavinton), a synthetic derivative of the Vinca minor alkaloid vincamine, has been used now for decades for prevention and treatment of cerebrovascular diseases predisposing to development of dementia. Both vinpoceti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63515a6447e002a84c81d8bfaa8d1f83
https://doi.org/10.1111/j.1755-5949.2009.00078.x
https://doi.org/10.1111/j.1755-5949.2009.00078.x