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

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 - Sep 2 2002

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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