1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists

A series of N,N′-diacylpiperazine-2-carboxamides are shown to be antagonists of the NK-1 (Substance P) receptor. Elaboration of the C2 sidechain with aminoalkyl groups leads to two series of potent antagonists, one containing simple dialkylamino groups and the second featuring 2-methoxybenzylamino d...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1993-12, Vol.3 (12), p.2707-2712
Main Authors: Mills, Sander G., Wu, Mu Tsu, MacCoss, Malcolm, Budhu, Richard J., Dorn, Conrad P., Cascieri, Margaret A., Sadowski, Sharon, Strader, Catherine D., Greenlee, William J.
Format: Article
Language:English
Subjects:
Analgesics
Biological and medical sciences
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
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Summary:A series of N,N′-diacylpiperazine-2-carboxamides are shown to be antagonists of the NK-1 (Substance P) receptor. Elaboration of the C2 sidechain with aminoalkyl groups leads to two series of potent antagonists, one containing simple dialkylamino groups and the second featuring 2-methoxybenzylamino derivatives with divergent SARs with respect to substitution at the C2 amide bond. A series of N,N′-diacylpiperazine-2-carboxamides are shown to be potent, selective antagonists of the NK-1 (Substance P) receptor.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80747-2