Discovery and Assessment of Atropisomers of (±)-Lesinurad
(+)- and (-)-Lesinurad were isolated as atropisomers from racemic lesinurad for the first time. No interconversion was observed between the two atropisomers under various conditions tested. The two atropisomers showed significant differences in hURAT1 highly expressed HEK293 cell-based inhibition assays, monkey pharmacokinetic studies, and in vitro human recombinant CYP2C9 stability studies. It was speculated that (+)-lesinurad might offer a better hyperuricemia/gout therapy than (-)-lesinurad or the racemate.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2017 |
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| Erschienen: |
2017 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:8 |
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| Enthalten in: |
ACS medicinal chemistry letters - 8(2017), 3 vom: 09. März, Seite 299-303 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Wang, Jianfei [VerfasserIn] |
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| Links: |
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| Themen: |
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| Anmerkungen: |
Date Revised 01.10.2020 published: Electronic-eCollection Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1021/acsmedchemlett.6b00465 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM270262091 |
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| 520 | |a (+)- and (-)-Lesinurad were isolated as atropisomers from racemic lesinurad for the first time. No interconversion was observed between the two atropisomers under various conditions tested. The two atropisomers showed significant differences in hURAT1 highly expressed HEK293 cell-based inhibition assays, monkey pharmacokinetic studies, and in vitro human recombinant CYP2C9 stability studies. It was speculated that (+)-lesinurad might offer a better hyperuricemia/gout therapy than (-)-lesinurad or the racemate | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Atropisomer | |
| 650 | 4 | |a gout | |
| 650 | 4 | |a hyperuricemia | |
| 650 | 4 | |a lesinurad | |
| 700 | 1 | |a Zeng, Wenqin |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Shaohua |e verfasserin |4 aut | |
| 700 | 1 | |a Shen, Liang |e verfasserin |4 aut | |
| 700 | 1 | |a Gu, Zhengxian |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Yang |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Jian |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Shuhui |e verfasserin |4 aut | |
| 700 | 1 | |a Jia, Xiangbo |e verfasserin |4 aut | |
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