Synthesis and Biological Studies of Novel Neurotensin(8–13) Mimetics

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• 作者：Hong ; Feng ; Zaidi ; Javid ; Cusack ; Bernadette ; Richelson ; Elliott
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2002
• 出版时间：December, 2002
• 年：2002
• 卷：10
• 期：12
• 页码：3849-3858
• 全文大小：216 K

文摘

Novel neurotensin (NT) (8–13) (Arg⁸-Arg⁹-Pro¹⁰-Tyr¹¹-Ile¹²-Leu¹³) mimetics 3, 4 were designed by adopting all intrinsic functional groups of the native neurotensin(8–13) and using a substituted indole as a template to mimic the pharmacophore of NT(8–13). Biological studies at subtype 1 of the NT receptor showed that 3 has a 55 and 580 nM binding affinity at rat and human neurotensin receptors, respectively. As a comparison, compounds 5 and 6 were also synthesized. The binding difference between 3, 4 and 5, 6 argues the importance of the carboxylic group in achieving higher potency NT(8–13) mimetics.