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Related Experiment Videos

Orally bioavailable competitive CCR5 antagonists.

Gebhard Thoma1, François Nuninger, Marc Schaefer

  • 1Novartis Institutes for BioMedical Research, Lichtstrasse 35, WSJ-507.4.12, CH-4056 Basel, Switzerland. gebhard.thoma@pharma.novartis.com

Journal of Medicinal Chemistry
|April 2, 2004
PubMed
Summary

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Researchers developed potent CCR5 antagonists for inflammatory diseases and HIV. One compound, 26n, shows promise for further study in animal models due to its effectiveness and favorable properties.

Area of Science:

  • Immunology
  • Pharmacology

Background:

  • Chemokine receptor CCR5 is crucial in inflammatory and autoimmune disorders, transplant rejection, and HIV infection.
  • CCR5 antagonists are potential therapeutics for these conditions.

Purpose of the Study:

  • To investigate the structure-activity relationship of novel, potent, and selective competitive CCR5 antagonists.
  • To identify compounds with potential for in vivo studies in disease models.

Main Methods:

  • Synthesis and testing of a new series of CCR5 antagonists.
  • Evaluation of compound activity on human and rodent CCR5 receptors.
  • Assessment of cross-reactivity with cynomolgus monkey CCR5.
  • Pharmacokinetic (PK) profiling of promising compounds in cynos.

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Main Results:

  • The series included highly potent and selective competitive CCR5 antagonists.
  • All tested compounds were inactive on rodent CCR5.
  • Some compounds demonstrated cross-reactivity with the cynomolgus monkey CCR5 receptor.
  • Compound 26n exhibited good PK properties in cynos and a favorable overall profile.

Conclusions:

  • The identified CCR5 antagonists represent a promising new class of therapeutics.
  • Compound 26n is a strong candidate for further in vivo evaluation in transplantation and other disease models.