5-Piperazinyl pyridine carboxamide bradykinin B₁ antagonists

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• 作者：Scott D. Kuduk ; Christina Ng Di Marco ; Ronald K. Chang ; Michael R. Wood ; June J. Kim ; Kathy M. Schirripa ; Kathy L. Murphy ; Richard W. Ransom ; Cuyue Tang ; Maricel Torrent et al.
• 关键词：Bradykinin B1 ; Antagonists ; Diaminopyridine ; Bioactivation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 May 2006
• 年：2006
• 卷：16
• 期：10
• 页码：2791-2795
• 全文大小：300 K

文摘

A series of 2,3-diaminopyridine bradykinin B₁ antagonists was modified to mitigate the potential for bioactivation. Removal of the 3-amino group and incorporation of basic 5-piperazinyl carboxamides at the pyridine 5-position provided compounds with high affinity for the human B₁ receptor.