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Novel pyrrolidine heterocycles as CCR1 antagonists

✍ Scribed by J. Robert Merritt; Ray James; Vidyadhar M. Paradkar; Chongwu Zhang; Ruiyan Liu; Jinqi Liu; Biji Jacob; Camelia Chiriac; Michael J. Ohlmeyer; Elizabeth Quadros; Pamela Wines; Jennifer Postelnek; Catherine M. Hicks; Weiqing Chen; Earl F. Kimble; Linda O’Brien; Nicole White; Hema Desai; Kenneth C. Appell; Maria L. Webb

Book ID
104004683
Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
239 KB
Volume
20
Category
Article
ISSN
0960-894X

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✦ Synopsis

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.

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