Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors

The NK1 and NK2 receptor activity of a series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4(Z)-(methoxyimino)pentyl-1-piperidines was evaluated. Compounds 11d, 11e, 11f, 12a, and 12k were found to be our most potent inhibitors.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-02, Vol.11 (4), p.491-494
Hauptverfasser:	TING, Pauline C, LEE, Joe F, ANTHES, John C, SHIH, Neng-Yang, PIWINSKI, John J
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Medical sciences Neurokinin-1 Receptor Antagonists Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - pharmacology Receptors, Neurokinin-2 - antagonists & inhibitors Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	The NK1 and NK2 receptor activity of a series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4(Z)-(methoxyimino)pentyl-1-piperidines was evaluated. Compounds 11d, 11e, 11f, 12a, and 12k were found to be our most potent inhibitors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00702-2