Département de Chimie, Université de Montréal , C.P. 6128, Succursale Centre-Ville, Montréal, Québec Canada H3C 3J7.
Org Lett. 2014 Apr 18;16(8):2232-5. doi: 10.1021/ol500739k. Epub 2014 Apr 4.
The synthesis of N-aminoimidazolidin-2-one (Aid) peptidomimetics has been achieved by alkylation of the urea nitrogen of a semicarbazone residue using ethylene bromide. The Aid scaffold combines electronic and structural constraints to rigidify the peptide backbone in the equivalent of an aza variant of a Freidinger-Veber lactam. The syntheses and isolation of 25 Aid peptides, including eight GHRP-6 analogues, are reported to demonstrate the utility of this method for controlling conformation.
已通过用溴化乙烯烷基化半缩酮残基上的脲氮来合成 N-氨甲酰基咪唑啉-2-酮（Aid）肽类似物。 Aid 支架结合了电子和结构约束，将肽主链固定在类似于 Freidinger-Veber 内酰胺的氮杂变体中。本文报道了 25 种 Aid 肽的合成和分离，其中包括 8 种 GHRP-6 类似物，以证明该方法在控制构象方面的实用性。
