Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome
Copyright © 2015 Elsevier Ltd. All rights reserved..
The synthesis, SAR, and in vivo activity of inhibitors of delta-5 desaturase are described. Ring-constraint of the initial series provided access to a variety of in vitro active chemotypes, from which the indazole was selected. Examples from the indazole series displayed in vivo activity in reducing the enzymatic activity of liver delta-5 desaturase.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2015 |
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| Erschienen: |
2015 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:25 |
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| Enthalten in: |
Bioorganic & medicinal chemistry letters - 25(2015), 18 vom: 15. Sept., Seite 3836-9 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Baugh, Simon D P [VerfasserIn] |
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| Links: |
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| Themen: |
Amides |
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| Anmerkungen: |
Date Completed 31.05.2016 Date Revised 03.12.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmcl.2015.07.066 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM251470784 |
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| 520 | |a Copyright © 2015 Elsevier Ltd. All rights reserved. | ||
| 520 | |a The synthesis, SAR, and in vivo activity of inhibitors of delta-5 desaturase are described. Ring-constraint of the initial series provided access to a variety of in vitro active chemotypes, from which the indazole was selected. Examples from the indazole series displayed in vivo activity in reducing the enzymatic activity of liver delta-5 desaturase | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Delta-5 desaturase | |
| 650 | 4 | |a In vivo efficacy | |
| 650 | 4 | |a Indazole | |
| 650 | 4 | |a Metabolic syndrome | |
| 650 | 4 | |a Ring constraint | |
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| 700 | 1 | |a Pabba, Praveen K |e verfasserin |4 aut | |
| 700 | 1 | |a Barbosa, Joseph |e verfasserin |4 aut | |
| 700 | 1 | |a Coulter, Eric |e verfasserin |4 aut | |
| 700 | 1 | |a Desai, Urvi |e verfasserin |4 aut | |
| 700 | 1 | |a Gay, Jason P |e verfasserin |4 aut | |
| 700 | 1 | |a Gopinathan, Suma |e verfasserin |4 aut | |
| 700 | 1 | |a Han, Qiang |e verfasserin |4 aut | |
| 700 | 1 | |a Hari, Rajee |e verfasserin |4 aut | |
| 700 | 1 | |a Kimball, S David |e verfasserin |4 aut | |
| 700 | 1 | |a Nguyen, Huy V |e verfasserin |4 aut | |
| 700 | 1 | |a Ni, Chi-You |e verfasserin |4 aut | |
| 700 | 1 | |a Powell, David R |e verfasserin |4 aut | |
| 700 | 1 | |a Smith, Arian |e verfasserin |4 aut | |
| 700 | 1 | |a Terranova, Kristen M |e verfasserin |4 aut | |
| 700 | 1 | |a Wilson, Alan |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Xuan-Chuan |e verfasserin |4 aut | |
| 700 | 1 | |a Lombardo, Victoria K |e verfasserin |4 aut | |
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