The P₁ N

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• 作者：Yasuchika Yamaguchi ; Keith Menear ; Nissim-Claude Cohen ; Robert Mah ; Fré ; dé ; ric Cumin ; Christian Schnell ; Jeanette M. Wood ; Jü ; rgen Maibaum
• 关键词：Renin– ; angiotensin– ; aldosterone system ; RAAS ; renin inhibitors ; Aliskiren analogues ; Hydroxyethylene dipeptide isosters
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：15 August 2009
• 年：2009
• 卷：19
• 期：16
• 页码：4863-4867
• 全文大小：363 K

文摘

Novel nonpeptide small molecule renin inhibitors bearing an N-isopropyl P₁ motif were designed based on initial lead structures 1 and aliskiren (2). (P₃–P₁)-Benzamide derivatives such as 9a and 34, as well as the corresponding P₁ basic tertiary amine derivatives 10 and 35 were found to display low nanomolar inhibition against human renin in vitro.