N-substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators
Copyright © 2010. Published by Elsevier Ltd..
A series of novel AMPA receptor positive modulators displaying CNS penetration have been discovered with sub-micromolar activity and good selectivity over the cardiac channel receptor, hERG. We describe here the synthesis of these compounds which are biaryl pyrrolidine and tetrahydrofuran sulfonamides and disclose their activities against the human GluA2 flip isoform homotetrameric receptor.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2010 |
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| Erschienen: |
2010 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:20 |
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| Enthalten in: |
Bioorganic & medicinal chemistry letters - 20(2010), 23 vom: 01. Dez., Seite 7116-9 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Thewlis, Kevin M [VerfasserIn] |
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| Links: |
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| Themen: |
ERG1 Potassium Channel |
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| Anmerkungen: |
Date Completed 23.02.2011 Date Revised 25.11.2016 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmcl.2010.09.062 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM202596869 |
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| 245 | 1 | 0 | |a N-substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators |
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| 500 | |a Date Revised 25.11.2016 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2010. Published by Elsevier Ltd. | ||
| 520 | |a A series of novel AMPA receptor positive modulators displaying CNS penetration have been discovered with sub-micromolar activity and good selectivity over the cardiac channel receptor, hERG. We describe here the synthesis of these compounds which are biaryl pyrrolidine and tetrahydrofuran sulfonamides and disclose their activities against the human GluA2 flip isoform homotetrameric receptor | ||
| 650 | 4 | |a Journal Article | |
| 650 | 7 | |a ERG1 Potassium Channel |2 NLM | |
| 650 | 7 | |a Ether-A-Go-Go Potassium Channels |2 NLM | |
| 650 | 7 | |a Furans |2 NLM | |
| 650 | 7 | |a KCNH2 protein, human |2 NLM | |
| 650 | 7 | |a Protein Isoforms |2 NLM | |
| 650 | 7 | |a Pyrrolidines |2 NLM | |
| 650 | 7 | |a Receptors, AMPA |2 NLM | |
| 650 | 7 | |a Sulfonamides |2 NLM | |
| 700 | 1 | |a Aldegheri, Laura |e verfasserin |4 aut | |
| 700 | 1 | |a Harries, Mark H |e verfasserin |4 aut | |
| 700 | 1 | |a Mookherjee, Claudette |e verfasserin |4 aut | |
| 700 | 1 | |a Oliosi, Beatrice |e verfasserin |4 aut | |
| 700 | 1 | |a Ward, Simon E |e verfasserin |4 aut | |
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