Sulfonamido-aryl ethers as bradykinin B1 receptor antagonists

Andrew G. Cole, Axel Metzger, Marc Raleigh Brescia, Lan Ying Qin, Kenneth C. Appell, Christopher T. Brain, Allan Hallett, Pam Ganju, Alastair A. Denholm, James R. Wareing, Timothy J. Ritchie, Gillian M. Drake, Stuart J. Bevan, Aisling MacGloinn, Andrew McBryde, Viral Patel, Paul J. Oakley, Ximena Nunez, Hubert Gstach, Peter SchneiderJohn J. Baldwin, Roland E. Dolle, Edward McDonald, Ian Henderson

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

The synthesis and identification of sulfonamido-aryl ethers as potent bradykinin B1 receptor antagonists from a ∼60,000 member encoded combinatorial library are reported. Two distinct series of compounds exhibiting different structure-activity relationships were identified in a bradykinin B1 whole-cell receptor-binding assay. Specific examples exhibit Ki values of ∼10 nM.

Original languageEnglish
Pages (from-to)119-122
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number1
DOIs
StatePublished - Jan 1 2009

Keywords

  • Bradykinin
  • Combinatorial chemistry
  • ECLiPS
  • Sulfonamide

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