The design and synthesis of novel NK1/NK2 dual antagonists

Functional probing of the backbone of the Sanofi NK2 antagonist SR 48968 has resulted in the discovery of two new classes of NK1/NK2 dual antagonists: the diamine class and the oxime class. The addition of the amino or the oxime functional group results in the reversal of the stereochemical preferen...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-10, Vol.10 (20), p.2329-2332
Hauptverfasser:	REICHARD, Gregory A, BALL, Zachary T, ASLANIAN, Robert, ANTHES, John C, SHIH, Neng-Yang, PIWINSKI, John J
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacology Biological and medical sciences Diamines - chemical synthesis Diamines - chemistry Diamines - pharmacology Drug Design Kinetics Medical sciences Molecular Structure Neurokinin-1 Receptor Antagonists Oximes - chemical synthesis Oximes - chemistry Oximes - pharmacology Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Receptors, Neurokinin-2 - antagonists & inhibitors Respiratory system Stereoisomerism Structure-Activity Relationship
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Zusammenfassung:	Functional probing of the backbone of the Sanofi NK2 antagonist SR 48968 has resulted in the discovery of two new classes of NK1/NK2 dual antagonists: the diamine class and the oxime class. The addition of the amino or the oxime functional group results in the reversal of the stereochemical preference of the NK2 receptor.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00463-7