Identification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists.

2.50
Hdl Handle:
http://hdl.handle.net/11287/619056
Title:
Identification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists.
Authors:
Allen, D. R.; Bolt, Amanda H. ( 0000-0003-4303-2718 ) ; Chapman, G. A.; Knight, R. L.; Meissner, J. W. G.; Owen, D. A.; Watson, R. J.
Abstract:
The synthesis and biological evaluation of a series of 1-aryl-3-piperidin-4-yl-urea derivatives as small-molecule CXCR3 antagonists is described. SAR studies resulted in significant improvement of potency and physicochemical properties and established the key pharmacophore of the series, and led to the identification of 9t, which exhibits an IC50 of 16 nM in the GTPgammaS35 functional assay.
Citation:
Identification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists. 2007, 17 (3):697-701 Bioorg. Med. Chem. Lett.
Publisher:
Elsevier
Journal:
Bioorganic & medicinal chemistry letters
Issue Date:
1-Feb-2007
URI:
http://hdl.handle.net/11287/619056
DOI:
10.1016/j.bmcl.2006.10.088
PubMed ID:
17097877
Additional Links:
http://www.sciencedirect.com/science/article/pii/S0960894X06012832
Note:
This article is freely available via Open Access. Click on the 'Additional Link' above to access the full-text from the publisher's site.
Type:
Journal Article
Language:
en
ISSN:
0960-894X
Appears in Collections:
pre-2014 RD&E publications

Full metadata record

DC FieldValue Language
dc.contributor.authorAllen, D. R.en
dc.contributor.authorBolt, Amanda H.en
dc.contributor.authorChapman, G. A.en
dc.contributor.authorKnight, R. L.en
dc.contributor.authorMeissner, J. W. G.en
dc.contributor.authorOwen, D. A.en
dc.contributor.authorWatson, R. J.en
dc.date.accessioned2016-08-30T10:23:14Z-
dc.date.available2016-08-30T10:23:14Z-
dc.date.issued2007-02-01-
dc.identifier.citationIdentification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists. 2007, 17 (3):697-701 Bioorg. Med. Chem. Lett.en
dc.identifier.issn0960-894X-
dc.identifier.pmid17097877-
dc.identifier.doi10.1016/j.bmcl.2006.10.088-
dc.identifier.urihttp://hdl.handle.net/11287/619056-
dc.description.abstractThe synthesis and biological evaluation of a series of 1-aryl-3-piperidin-4-yl-urea derivatives as small-molecule CXCR3 antagonists is described. SAR studies resulted in significant improvement of potency and physicochemical properties and established the key pharmacophore of the series, and led to the identification of 9t, which exhibits an IC50 of 16 nM in the GTPgammaS35 functional assay.en
dc.language.isoenen
dc.publisherElsevieren
dc.relation.urlhttp://www.sciencedirect.com/science/article/pii/S0960894X06012832en
dc.rightsArchived with thanks to Bioorganic & medicinal chemistry lettersen
dc.subjectWessex Classification Subject Headings::Biochemistryen
dc.titleIdentification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists.en
dc.typeJournal Articleen
dc.identifier.journalBioorganic & medicinal chemistry lettersen
dc.description.noteThis article is freely available via Open Access. Click on the 'Additional Link' above to access the full-text from the publisher's site.en
dc.type.versionPublisheden

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