公开(公告)号：US06797829B1

公开(公告)日：2004-09-28

申请号：US10018842

申请日：2001-12-21

申请人： Clóvis Ryuichi Nakaie ,  Mineko Tominaga ,  Antonio Cechlli Matto Paiva ,  Simone dos Reis Barbosa ,  Reinaldo Machetto ,  Shirley Schreier

发明人： Clóvis Ryuichi Nakaie ,  Mineko Tominaga ,  Antonio Cechlli Matto Paiva ,  Simone dos Reis Barbosa ,  Reinaldo Machetto ,  Shirley Schreier

IPC分类号： C07D20746

CPC分类号： C07D207/46 ,  Y02P20/55

摘要： The present invention refers to the synthesis and application of 2,2,5,5-tetramethylpyrrolidine-N-oxyl-(9-fluorenylmethyloxycarbonyl)-3-amine-4-carboxylic acid, a novel paramagnetic amino acid derivative (spin label), denominated Fmoc-Poac. Fmoc-Poac can be coupled to peptide sequences and other molecules or systems. It can be inserted anywhere in a peptide segment, even at an internal position if necessary, after removal of its temporary amine protecting group, Fmoc. Owing to its pyrrolidine structure, this molecule may induce differentiated conformations as compared with normal &agr;-amino acids, thus being a valuable probe for structural-biological activity of several relevant peptides. The Poac-angiotensin II analogue was synthesized as a model according to its use as a chemical derivative.

摘要翻译： 本发明涉及2,2,5,5-四甲基吡咯烷-N-氧基 - （9-芴基甲氧基羰基）-3-胺-4-羧酸（新型顺磁性氨基酸衍生物（自旋标记））的合成和应用， 称为Fmoc-Poac。 Fmoc-Poac可以与肽序列和其他分子或系统偶联。 除去其临时胺保护基团Fmoc之外，如果需要，它可以插入肽段的任何地方，甚至在内部位置。 由于其吡咯烷结构，与正常的α-氨基酸相比，该分子可诱导分化的构象，因此是几种相关肽的结构 - 生物活性的有价值的探针。 根据其作为化学衍生物的用途合成了Poac-血管紧张素II类似物作为模型。