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Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Jan 01; Vol. 16 (1), pp. 200-3. Date of Electronic Publication: 2005 Oct 05. - Publication Year :
- 2006
-
Abstract
- The identification and evaluation of aryl-[1,4]diazepane ureas as functional antagonists of the chemokine receptor CXCR3 are described. Specific examples exhibit IC(50) values of approximately 60 nM in a calcium mobilization functional assay, and dose-dependently inhibit CXCR3 functional response to CXCL11 (interferon-inducible T-cell alpha chemoattractant/I-TAC) as measured by T-cell chemotaxis, with a potency of approximately 100 nM.
- Subjects :
- Calcium metabolism
Cell Line
Chemistry, Pharmaceutical methods
Chemokine CXCL11
Chemokines, CXC chemistry
Chemotaxis
Dose-Response Relationship, Drug
Drug Design
Drug Evaluation, Preclinical
Electrons
Humans
Inflammation
Inhibitory Concentration 50
Models, Chemical
Receptors, CXCR3
Receptors, Chemokine chemistry
Receptors, G-Protein-Coupled metabolism
Recombinant Proteins chemistry
Stereoisomerism
T-Lymphocytes cytology
Receptors, Chemokine antagonists & inhibitors
Urea chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16213722
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.09.020