4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase
4-(1,1-Dioxo-1,4-dihydro-1lambda(6)-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-one analogs were discovered as a novel class of inhibitors of HCV NS5B polymerase. Structure-based design led to the identification of compound 3a that displayed potent inhibitory activities in biochemical and replicon assays (1b IC(50)<10 nM; 1b EC(50)=1.1 nM) as well as good stability toward human liver microsomes (HLM t(1/2)>60 min).
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2008 |
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| Erschienen: |
2008 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:18 |
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| Enthalten in: |
Bioorganic & medicinal chemistry letters - 18(2008), 16 vom: 15. Aug., Seite 4628-32 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ellis, David A [VerfasserIn] |
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| Links: |
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| Themen: |
EC 2.7.7.48 |
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| Anmerkungen: |
Date Completed 24.11.2008 Date Revised 10.01.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmcl.2008.07.014 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM181220911 |
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| 100 | 1 | |a Ellis, David A |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a 4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase |
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| 520 | |a 4-(1,1-Dioxo-1,4-dihydro-1lambda(6)-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-one analogs were discovered as a novel class of inhibitors of HCV NS5B polymerase. Structure-based design led to the identification of compound 3a that displayed potent inhibitory activities in biochemical and replicon assays (1b IC(50)<10 nM; 1b EC(50)=1.1 nM) as well as good stability toward human liver microsomes (HLM t(1/2)>60 min) | ||
| 650 | 4 | |a Journal Article | |
| 650 | 7 | |a Pyridazines |2 NLM | |
| 650 | 7 | |a Thiazines |2 NLM | |
| 650 | 7 | |a Viral Nonstructural Proteins |2 NLM | |
| 650 | 7 | |a NS-5 protein, hepatitis C virus |2 NLM | |
| 650 | 7 | |a EC 2.7.7.48 |2 NLM | |
| 700 | 1 | |a Blazel, Julie K |e verfasserin |4 aut | |
| 700 | 1 | |a Webber, Stephen E |e verfasserin |4 aut | |
| 700 | 1 | |a Tran, Chinh V |e verfasserin |4 aut | |
| 700 | 1 | |a Dragovich, Peter S |e verfasserin |4 aut | |
| 700 | 1 | |a Sun, Zhongxiang |e verfasserin |4 aut | |
| 700 | 1 | |a Ruebsam, Frank |e verfasserin |4 aut | |
| 700 | 1 | |a McGuire, Helen M |e verfasserin |4 aut | |
| 700 | 1 | |a Xiang, Alan X |e verfasserin |4 aut | |
| 700 | 1 | |a Zhao, Jingjing |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Lian-Sheng |e verfasserin |4 aut | |
| 700 | 1 | |a Zhou, Yuefen |e verfasserin |4 aut | |
| 700 | 1 | |a Han, Qing |e verfasserin |4 aut | |
| 700 | 1 | |a Kissinger, Charles R |e verfasserin |4 aut | |
| 700 | 1 | |a Showalter, Richard E |e verfasserin |4 aut | |
| 700 | 1 | |a Lardy, Matthew |e verfasserin |4 aut | |
| 700 | 1 | |a Shah, Amit M |e verfasserin |4 aut | |
| 700 | 1 | |a Tsan, Mei |e verfasserin |4 aut | |
| 700 | 1 | |a Patel, Rupal |e verfasserin |4 aut | |
| 700 | 1 | |a LeBrun, Laurie A |e verfasserin |4 aut | |
| 700 | 1 | |a Kamran, Ruhi |e verfasserin |4 aut | |
| 700 | 1 | |a Bartkowski, Darian M |e verfasserin |4 aut | |
| 700 | 1 | |a Nolan, Thomas G |e verfasserin |4 aut | |
| 700 | 1 | |a Norris, Daniel A |e verfasserin |4 aut | |
| 700 | 1 | |a Sergeeva, Maria V |e verfasserin |4 aut | |
| 700 | 1 | |a Kirkovsky, Leo |e verfasserin |4 aut | |
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