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Potent small molecule CCR1 antagonists.

John C Kath1, William H Brissette, Matthew F Brown

  • 1Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA. john_c_kath@groton.pfizer.com

Bioorganic & Medicinal Chemistry Letters
|April 15, 2004
PubMed
Summary
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Structure-activity relationship studies identified novel chemokine (CC) receptor 1 (CCR1) antagonists. These new compounds are over 100 times more potent than the original lead compound 1.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology

Background:

  • Chemokine (CC) receptor 1 (CCR1) is a key target in inflammatory diseases.
  • Lead compound 1 showed initial CCR1 antagonist activity.

Purpose of the Study:

  • To optimize lead compound 1 through structure-activity relationship (SAR) studies.
  • To discover novel, highly potent CCR1 antagonists.

Main Methods:

  • Systematic chemical modification of lead compound 1.
  • In vitro assays to evaluate CCR1 antagonist potency and activity.

Main Results:

  • Detailed SAR insights were obtained for the lead structure.
  • Discovery of novel CCR1 antagonists with >100-fold increased potency compared to compound 1.

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Conclusions:

  • Successful optimization of lead compound 1 yielded significantly more potent CCR1 antagonists.
  • These findings provide a strong foundation for developing new CCR1-targeted therapeutics.