Piperazinyl oxime ethers as NK-1 receptor antagonists

The synthesis and SAR for a new class of centrally active NK-1 receptor antagonists are described. The new compounds all have a piperazinyl 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....

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-02, Vol.16 (4), p.1045-1048
Hauptverfasser:	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.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Anti-Anxiety Agents - administration & dosage Anti-Anxiety Agents - chemical synthesis Anti-Anxiety Agents - pharmacology Biological and medical sciences CHO Cells Cricetinae Drug Evaluation, Preclinical Ethers - administration & dosage Ethers - chemical synthesis Ethers - pharmacology Gerbillinae Humans Medical sciences Molecular Conformation Motor Activity - drug effects Neurokinin Neurokinin-1 Receptor Antagonists Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oxime ethers Oximes - administration & dosage Oximes - chemical synthesis Oximes - pharmacology Peptide Fragments - antagonists & inhibitors Peptide Fragments - pharmacology Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Piperazines - administration & dosage Piperazines - chemical synthesis Piperazines - pharmacology SAR Structure-Activity Relationship Substance P - analogs & derivatives Substance P - antagonists & inhibitors Substance P - pharmacology Synthesis
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Beschreibung
Zusammenfassung:	The synthesis and SAR for a new class of centrally active NK-1 receptor antagonists are described. The new compounds all have a piperazinyl 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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.10.077