Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions

Ho Jane Shue, Xiao Chen, John H. Schwerdt, Sunil Paliwal, David J. Blythin, Ling Lin, Danlin Gu, Cheng Wang, Gregory A. Reichard, Hongwu Wang, John J. Piwinski, Ruth A. Duffy, Jean E. Lachowicz, Vicki L. Coffin, Amin A. Nomeir, Cynthia A. Morgan, Geoffrey B. Varty, Neng Yang Shih

Research output: Contribution to journalArticlepeer-review

26 Scopus citations

Abstract

A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an α-methyl group at the benzylic position to improve potency and duration of in vivo activity are discussed. Several compounds with high affinity and sustained in vivo activity were identified.

Original languageEnglish
Pages (from-to)1065-1069
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number4
DOIs
StatePublished - 15 Feb 2006

Keywords

  • Improved potency
  • NK antagonist
  • Sustained in vivo activity

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