化学
环丁烷
立体化学
体外
化学合成
受体
NK1受体拮抗剂
结构-活动关系
药理学
生物化学
戒指(化学)
有机化学
神经肽
医学
P物质
作者
Michelle Laci Wrobleski,Gregory A. Reichard,Sunil Paliwal,Sapna Shah,Hon‐Chung Tsui,Ruth A. Duffy,Jean E. Lachowicz,Cynthia A. Morgan,Geoffrey B. Varty,Neng‐Yang Shih
标识
DOI:10.1016/j.bmcl.2006.04.031
摘要
A series of novel cyclobutane derivatives as potent and selective NK1 receptor antagonists is described. Several compounds in this series exhibited high in vitro binding affinity (Ki ⩽ 1 nM), and potent inhibition of central NK1 receptor following oral administration. Syntheses of these compounds are also described herein.
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