Peer-reviewed veterinary case report
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2007
- Authors:
- Xie, Yun Feng et al.
- Affiliation:
- Department of Chemistry · United States
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.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/17446072/