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Piperazinyl oxime ethers as NK-1 receptor antagonists.

Bioorganic & medicinal chemistry letters (2005-11-18)
Adri van den Hoogenband, Jan H van Maarseveen, Andrew C McCreary, Arie T Mulder, Guus J M van Scharrenburg, Herman H van Stuivenberg, Theo J J Zethof, Barbara Zijta, Wouter I Iwema Bakker
PMID16289817
ABSTRACT

The synthesis and structure-activity relations for a new class of centrally active NK-1 receptor antagonists are described. The new compounds are based on piperazine 2 and contain an oxime ether functionality. Several new compounds have high affinity for the NK-1 receptor and show good antagonistic activity in the gerbil foot-tapping assay.