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Highly potent, orally available anti-inflammatory broad-spectrum chemokine inhibitors
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Fox, David J., Reckless, Jill, Lingard, Hannah, Warren, Stuart and Grainger, David J. (2009) Highly potent, orally available anti-inflammatory broad-spectrum chemokine inhibitors. Journal of Medicinal Chemistry, Vol.52 (No.11). pp. 3591-3595. doi:10.1021/jm900133w ISSN 0022-2623.
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Official URL: http://dx.doi.org/10.1021/jm900133w
Abstract
A series of 3-acylaminocaprolactams are inhibitors of chemokine-induced chemotaxis. Branching of the side chain alpha-carbon provides highly potent inhibitors of a range of CC and CXC chemokines. The most potent compound has an ED50 of 40 pM. Selected compounds were tested in an in vivo inflammatory assay, and the best compound reduces TNF-alpha levels with an ED50 of 0.1 mu g/kg when administered by either subcutaneous injection or oral delivery.
Item Type: | Journal Article | ||||
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Subjects: | Q Science > QD Chemistry | ||||
Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry | ||||
Journal or Publication Title: | Journal of Medicinal Chemistry | ||||
Publisher: | American Chemical Society | ||||
ISSN: | 0022-2623 | ||||
Official Date: | 11 June 2009 | ||||
Dates: |
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Volume: | Vol.52 | ||||
Number: | No.11 | ||||
Number of Pages: | 5 | ||||
Page Range: | pp. 3591-3595 | ||||
DOI: | 10.1021/jm900133w | ||||
Status: | Peer Reviewed | ||||
Publication Status: | Published | ||||
Access rights to Published version: | Restricted or Subscription Access | ||||
Funder: | Dr John Davies for crystallography, Engineering and Physical Sciences Research Council (EPSRC) |
Data sourced from Thomson Reuters' Web of Knowledge
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