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

Fingerprint

Dive into the research topics of 'Preparation of oxime dual NK1/NK2 antagonists with reduced NK3 affinity'. Together they form a unique fingerprint.

Cite this