Highly Potent, Orally Available Anti-inflammatory Broad-Spectrum Chemokine Inhibitors
Journal of Medicinal Chemistry2009Vol. 52(11), pp. 3591–3595
Citations Over TimeTop 23% of 2009 papers
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 ED(50) of 40 pM. Selected compounds were tested in an in vivo inflammatory assay, and the best compound reduces TNF-alpha levels with an ED(50) of 0.1 microg/kg when administered by either subcutaneous injection or oral delivery.
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