The tandem chain extension aldol reaction used for synthesis of ketomethylene tripeptidomimetics targeting hPEPT1

K Thorn, CU Nielsen, P Jakobsen, B Steffansen…

文献索引：Thorn, Karina; Nielsen, Carsten Uhd; Jakobsen, Palle; Steffansen, Bente; Zercher, Charles K.; Begtrup, Mikael Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 15 p. 4597 - 4601

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被引用次数: 2

摘要

The rationale for targeting the human di-/tripeptide transporter hPEPT1 for oral drug delivery has been well established by several drug and prodrug cases. The aim of this study was to synthesize novel ketomethylene modified tripeptidomimetics and to investigate their binding affinity for hPEPT1. Three related tripeptidomimetics of the structure H-Phe-ψ [COCH2]-Ser (Bz)-Xaa-OH were synthesized applying the tandem chain extension aldol reaction, where ...