Preparation of oxime dual NK1/NK2 antagonists with reduced NK3 affinity

  • Gregory A. Reichard
  • , Cheryl A. Grice
  • , Neng Yang Shih
  • , James Spitler
  • , Sapna Majmundar
  • , Steven D. Wang
  • , Sunil Paliwal
  • , John C. Anthes
  • , John J. Piwinski

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

By employing a stereosimplification approach, a thorough SAR exploration of the piperidine region of Sch 206272 was possible through a practical and efficient synthesis of substituted cyclic ureas. This SAR study led to the identification of a benzimidazolinone series of compounds which display single digit nanomolar NK1/NK2 affinity and near micromolar binding for the NK3 receptor.

Original languageEnglish
Pages (from-to)2355-2358
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number17
DOIs
StatePublished - 2 Sep 2002

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