Cyclobutane derivatives as potent NK sub(1) selective antagonists

Cyclobutane derivatives as potent NK sub(1) selective antagonists

A series of novel cyclobutane derivatives as potent and selective NK sub(1) receptor antagonists is described. Several compounds in this series exhibited high in vitro binding affinity (K sub(i) 1 nM), and potent inhibition of central NK sub(1) receptor following oral administration. Syntheses of th...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (14), p.3859-3863
Hauptverfasser: Wrobleski, Michelle Laci, Reichard, Gregory A, Paliwal, Sunil, Shah, Sapna, Tsui, Hon-Chung, Duffy, Ruth A, Lachowicz, Jean E, Morgan, Cynthia A, Varty, Geoffrey B, Shih, Neng-Yang
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Sprache:eng
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Zusammenfassung:A series of novel cyclobutane derivatives as potent and selective NK sub(1) receptor antagonists is described. Several compounds in this series exhibited high in vitro binding affinity (K sub(i) 1 nM), and potent inhibition of central NK sub(1) receptor following oral administration. Syntheses of these compounds are also described herein.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.04.031