New sst4/5-Selective Somatostatin Peptidomimetics Based on a Constrained Tryptophan Scaffold

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• 作者：Debby Feytens ; Renzo Cescato ; Jean Claude Reubi ; Dirk Tourwé
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：July 12, 2007
• 年：2007
• 卷：50
• 期：14
• 页码：3397 - 3401
• 全文大小：96K
• 年卷期：v.50,no.14(July 12, 2007)
• ISSN：1520-4804

文摘

The synthesis and biological evaluation of four peptidomimetic analogs of somatostatin based on a constrainedTrp residue, 3-amino-indolo[2,3-c]azepin-2-one (Aia), are reported. It is shown that dipeptidomimetics witha D-Aia-Lys sequence, functionalized with N- and C-terminal aromatic substituents, display a good selectivityfor both sst₄ and sst_5. This study allowed us to identify a new highly potent sst₅ agonist with good selectivityover the other receptors, except versus sst₄.