Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1864-8. doi: 10.1016/j.bmcl.2008.02.010. Epub 2008 Feb 10.

Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.

Author information

1
Pharmacopeia, Inc., 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA. galai@pcop.com

Abstract

A series of 3,4- and 3,5-disubstituted phenyl-containing cyclobutenedione analogues were synthesized and evaluated as CXCR2 receptor antagonists. Variations in the disubstitution pattern of the phenyl ring afforded new compounds with potent CXCR2 binding affinity in the low nanomolar ranges. Moreover, two potent compounds 19 and 26 exhibited good oral pharmacokinetic profiles.

PMID:
18304809
DOI:
10.1016/j.bmcl.2008.02.010
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center