2. Academic Validation
  3. Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists

Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists

  • Bioorg Med Chem Lett. 2007 Jun 15;17(12):3367-72. doi: 10.1016/j.bmcl.2007.03.104.
Yun Feng Xie 1,  Kirk Lake,  Kathleen Ligsay,  Mallareddy Komandla,  Ila Sircar,  Gobi Nagarajan,  Jian Li,  Kui Xu,  Jason Parise,  Lisa Schneider,  Ding Huang,  Juping Liu,  Kevin Dines,  Naoki Sakurai,  Miguel Barbosa,  Rick Jack
Affiliations

Affiliation

  • 1 Department of Chemistry, Tanabe Research Laboratories, Inc., 4540 Towne Centre Court, San Diego, CA 92121, USA.
PMID: 17446072 DOI: 10.1016/j.bmcl.2007.03.104
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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