Discovery of a series of potent, orally active α,α-disubstituted piperidine NK₁ antagonists

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• 作者：Dong Xiao ; Cheng Wang ; An ; an Palani ; Hon-Chung Tsui ; Gregory Reichard ; Sunil Paliwal ; Neng-Yang Shih ; Robert Aslanian ; Ruth Duffy ; Jean Lachowicz ; Geoffrey Varty ; Cynthia Morgan ; Fei Liu ; Amin Nomeir
• 关键词：NK₁ antagonist ; Dibasic amine metabolite
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 November 2010
• 年：2010
• 卷：20
• 期：21
• 页码：6313-6315
• 全文大小：1337 K

文摘

Modification of prototype NK₁ antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK₁ antagonists.