III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold
Copyright © 2011 Elsevier Ltd. All rights reserved..
The SAR of a novel pyrazinyl-piperazinyl-piperidine scaffold with CXCR3 receptor antagonist activity was explored. Optimization of the DMPK profile and reduction of hERG inhibition is described. Compound 16e with single-digit CXCR3 affinity, good rat PK and hERG profiles has been identified as a lead for further study.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2011 |
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| Erschienen: |
2011 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:21 |
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| Enthalten in: |
Bioorganic & medicinal chemistry letters - 21(2011), 23 vom: 01. Dez., Seite 6982-6 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Kim, Seong Heon [VerfasserIn] |
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| Links: |
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| Themen: |
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| Anmerkungen: |
Date Completed 18.04.2012 Date Revised 07.11.2011 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmcl.2011.09.120 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM212414267 |
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| 245 | 1 | 0 | |a III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2011 Elsevier Ltd. All rights reserved. | ||
| 520 | |a The SAR of a novel pyrazinyl-piperazinyl-piperidine scaffold with CXCR3 receptor antagonist activity was explored. Optimization of the DMPK profile and reduction of hERG inhibition is described. Compound 16e with single-digit CXCR3 affinity, good rat PK and hERG profiles has been identified as a lead for further study | ||
| 650 | 4 | |a Journal Article | |
| 650 | 7 | |a Piperazines |2 NLM | |
| 650 | 7 | |a Pyrazines |2 NLM | |
| 650 | 7 | |a Receptors, CXCR3 |2 NLM | |
| 700 | 1 | |a Anilkumar, Gopinadhan N |e verfasserin |4 aut | |
| 700 | 1 | |a Zawacki, Lisa Guise |e verfasserin |4 aut | |
| 700 | 1 | |a Zeng, Qingbei |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, De-Yi |e verfasserin |4 aut | |
| 700 | 1 | |a Shao, Yuefei |e verfasserin |4 aut | |
| 700 | 1 | |a Dong, Guizhen |e verfasserin |4 aut | |
| 700 | 1 | |a Xu, Xiaolian |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Wensheng |e verfasserin |4 aut | |
| 700 | 1 | |a Jiang, Yueheng |e verfasserin |4 aut | |
| 700 | 1 | |a Jenh, Chung-Her |e verfasserin |4 aut | |
| 700 | 1 | |a Hall, James W |c 3rd |e verfasserin |4 aut | |
| 700 | 1 | |a Carroll, Carolyn Diianni |e verfasserin |4 aut | |
| 700 | 1 | |a Hobbs, Doug W |e verfasserin |4 aut | |
| 700 | 1 | |a Baldwin, John J |e verfasserin |4 aut | |
| 700 | 1 | |a McGuinness, Brian F |e verfasserin |4 aut | |
| 700 | 1 | |a Rosenblum, Stuart B |e verfasserin |4 aut | |
| 700 | 1 | |a Kozlowski, Joseph A |e verfasserin |4 aut | |
| 700 | 1 | |a Shankar, Bandarpalle B |e verfasserin |4 aut | |
| 700 | 1 | |a Shih, Neng-Yang |e verfasserin |4 aut | |
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