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Highly Potent, Orally Available Anti-inflammatory Broad-Spectrum Chemokine Inhibitors
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Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K., Department of Medicine, University of Cambridge, Box 157, Addenbrooke’s Hospital, Cambridge CB2 2QQ, U.K.
J. Med. Chem., 2009, 52 (11), pp 3591–3595
DOI: 10.1021/jm900133w
Publication Date (Web): May 8, 2009
Copyright © 2009 American Chemical Society
* To whom correspondence should be addressed. Phone: +44 (0)24 7652 4331. Fax: +44 (0)24 7652 4112. E-mail: d.j.fox@warwick.ac.uk., †
Department of Chemistry, University of Cambridge.
, ‡Department of Medicine, University of Cambridge.
, §Current Address: Department of Chemistry, University of Warwick, Gibbet Hill Road, Coventry, CV4 7AL, U.K.
Section:Abstract
A series of 3-acylaminocaprolactams are inhibitors of chemokine-induced chemotaxis. Branching of the side chain α-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-α levels with an ED50 of 0.1 μg/kg when administered by either subcutaneous injection or oral delivery.
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History
- Published In Issue June 11, 2009
- Article ASAPMay 08, 2009
- Received: February 3, 2009
ACS
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