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Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jun 15; Vol. 17 (12), pp. 3367-72. Date of Electronic Publication: 2007 Apr 05. - Publication Year :
- 2007
-
Abstract
- Design and synthesis of a series of 3-amino-4-(2-(2-(4-benzylpiperazin-1-yl)-2-oxoethoxy)phenylamino)cyclobutenedione derivatives as novel CCR1 antagonists are described. Structure-activity relationship studies led to the identification of compound 22, which demonstrated potent binding activity, functional antagonism of CCR1 as well as good species cross-reactivity. In addition, compound 22 also showed desirable pharmacokinetic profiles and was selected for in vivo studies in the mouse collagen-induced arthritis model.
- Subjects :
- Administration, Oral
Animals
Arthritis, Experimental chemically induced
Benzyl Compounds chemistry
Binding Sites
Collagen
Cyclobutanes chemistry
Disease Models, Animal
Drug Design
Male
Mice
Mice, Inbred BALB C
Receptors, CCR1
Structure-Activity Relationship
Arthritis, Experimental drug therapy
Benzyl Compounds pharmacology
Cyclobutanes pharmacology
Receptors, Chemokine antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17446072
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.03.104