Catechol: A Minimal Scaffold for Non-Peptide Peptidomimetics of the i + 1 and i + 2 Positions of the -T

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• 作者：Brendan P. Mowery ; Vidya Prasad ; Craig S. Kenesky ; Angie R. Angeles ; Laurie L. Taylor ; Jin-Jye Feng ; Wen-Long Chen ; Atsui Lin ; Fong-Chi Cheng ; Amos B. Smith ; III ; Ralph Hirschmann
• 刊名：Organic Letters
• 出版年：2006
• 出版时间：September 28, 2006
• 年：2006
• 卷：8
• 期：20
• 页码：4397 - 4400
• 全文大小：130K
• 年卷期：v.8,no.20(September 28, 2006)
• ISSN：1523-7052

文摘

The design, synthesis, and evaluation of a series of catechol-based non-peptide peptidomimetics of the peptide hormone somatostatin havebeen achieved. These ligands comprise the simplest known non-peptide mimetics of the i + 1 and i + 2 positions of the somatostatin -turn.Incorporation of an additional side chain to include the i position of the -turn induces a selective 9-fold affinity enhancement at the sst₂receptor.