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Bioorg Med Chem Lett. 2002 Sep 2;12(17):2355-8.

Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.

Author information

1
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. gregory.reichard@spcorp.com

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 NK(1)/NK(2) affinity and near micromolar binding for the NK(3) receptor.

PMID:
12161132
DOI:
10.1016/s0960-894x(02)00462-6
[Indexed for MEDLINE]

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