Novel pyrrolidine heterocycles as CCR1 antagonists.

  title={Novel pyrrolidine heterocycles as CCR1 antagonists.},
  author={J Robert Merritt and Ray James and Vidyadhar M Paradkar and Chongwu Zhang and Ruiyan Liu and Jinqi Liu and Biji Jacob and Camelia Chiriac and Michael H J Ohlmeyer and Elizabeth Quadros and Pamela G Wines and Jennifer Postelnek and Catherine M. Hicks and Weiqing Chen and Earl F. Kimble and Linda O'Brien and Nicole White and Hema Desai and Kenneth C. Appell and M. L. Webb},
  journal={Bioorganic & medicinal chemistry letters},
  volume={20 18},
A novel series of pyrrolidine heterocycles was prepared and found to show potent inhibitory activity of CCR1 binding and CCL3 mediated chemotaxis of a CCR1-expressing cell line. A potent, optimized triazole lead from this series was found to have acceptable pharmacokinetics and microsomal stability in rat and is suitable for further optimization and development.