Synthesis and evaluation of isoleucine derived angiotensin II AT₂ receptor ligands

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• 作者：Jean-Baptiste Veron ; Advait Joshi ; Charlotta Wallinder ; Mats Larhed ; Luke R. Odell
• 关键词：AT2 receptor ; AT1 receptor ; Angiotensin ; Isoleucine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 January, 2014
• 年：2014
• 卷：24
• 期：2
• 页码：476-479
• 全文大小：1828 K

文摘

Sixteen new C-terminally modified analogues of 2, a previously described potent and selective AT₂R ligand, were designed, synthesized and evaluated for their affinity to the AT₂R receptor. The introduction of large, hydrophobic substituents was shown to be beneficial and the most active compound (17, K_i = 8.5 渭M) was over 12-times more potent than the lead compound 2.