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Piperazinyl oxime ethers as NK-1 receptor antagonists.

van den Hoogenband, Adri; van Maarseveen, Jan H; McCreary, Andrew C; Mulder, Arie T; van Scharrenburg, Guus J M; van Stuivenberg, Herman H; Zethof, Theo J J; Zijta, Barbara; Iwema Bakker, Wouter I.

Bioorg Med Chem Lett ; 16(4): 1045-8, 2006 Feb 15.

Article in English | MEDLINE | ID: mdl-16289817

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.

Subject(s)

Anti-Anxiety Agents/pharmacology , Ethers/pharmacology , Neurokinin-1 Receptor Antagonists , Oximes/pharmacology , Piperazines/pharmacology , Administration, Oral , Animals , Anti-Anxiety Agents/administration & dosage , Anti-Anxiety Agents/chemical synthesis , CHO Cells , Cricetinae , Drug Evaluation, Preclinical , Ethers/administration & dosage , Ethers/chemical synthesis , Gerbillinae , Humans , Molecular Conformation , Motor Activity/drug effects , Oximes/administration & dosage , Oximes/chemical synthesis , Peptide Fragments/antagonists & inhibitors , Peptide Fragments/pharmacology , Piperazines/administration & dosage , Piperazines/chemical synthesis , Structure-Activity Relationship , Substance P/analogs & derivatives , Substance P/antagonists & inhibitors , Substance P/pharmacology

ABSTRACT

Subject(s)

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