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Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
18
Issue
17
Identifiers
DOI: 10.1016/j.bmcl.2008.07.108
Keywords
  • Bradykinin Antagonist
  • Chronic Pain
  • Aryl Sulfone
Disciplines
  • Chemistry
  • Medicine

Abstract

Abstract We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modifications of the aryl moiety led to compound 26, both of which were efficacious in rabbit biochemical challenge and pain models.

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