Výsledky vyhledávání - "György Domány"

Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators

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

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

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Thieno[2,3- b ]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization

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

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Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu

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

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Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Hit-to-lead optimization

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

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Design of novel multiple-acting ligands towards SERT and 5-HT2C receptors

Autor: Istvan Gyertyan, Éva Hellinger, Mónika Vastag, Éva Ágai-Csongor, Olivér Éliás, György Domány, Bela Kiss, Aniko Gere, György M. Keserű

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:2118-2122

This Letter describes our attempts to elaborate dually acting compounds possessing serotonin re-uptake transporter inhibitor and serotonin 5-HT2C receptor antagonist properties. A novel series of 1,3-diphenylureas and N-phenylbenzamides have thus bee

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62e4100a1566d614d99a3d992309a973
https://doi.org/10.1016/j.bmcl.2014.03.043

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4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors:From HTS hit to development candidate

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

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

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Discovery of cariprazine (RGH-188): A novel antipsychotic acting on dopamine D3/D2 receptors

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

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Synthesis of deuterated dextromethorphan derivatives

Autor: Ferencz Dravecz, Hedvig Bölcskei, György Domány, Marianna Mák

Publikováno v: ARKIVOC, Vol 2008, Iss 3, Pp 182-193 (2008)

Dextromethorphan is a widely used NMDA receptor antagonist and sodium channel blocker. Deuterated dextromethorphan and dextrorphan were synthesized via the N-desmethyl- dextromethorphan intermediate for pharmacokinetic study.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3440d41b43a46c905b62bcf3f9d698d
https://www.arkat-usa.org/arkivoc-journal/browse-arkivoc/ark.5550190.0009.316

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