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基于 AAZTA 的双功能螯合剂用于合成多聚体/树枝状 MRI 造影剂。

AAZTA-based bifunctional chelating agents for the synthesis of multimeric/dendrimeric MRI contrast agents.

机构信息

Dipartimento di Scienze dell'Ambiente e della Vita, Università del Piemonte Orientale Amedeo Avogadro, Viale T. Michel 11, 15121, Alessandria, Italy.

出版信息

Org Biomol Chem. 2010 Oct 21;8(20):4569-74. doi: 10.1039/c0ob00096e. Epub 2010 Aug 25.

Abstract

Monomeric and dimeric bifunctional chelates based on the AAZTA (6-amino-6-methylperhydro-1,4-diazepinetetraacetic acid) platform bearing arylamino and isothiocyanate groups for conjugation to biomolecules were synthesised. Both systems were used for the preparation of high relaxivity dendrimeric (PAMAM G1) and multimeric octa-Gd(III) complexes. These systems show enhanced relaxometric properties attributed to the presence of two coordinated, fast exchanging, water molecules (q = 2) on each metal ion and to a rather rigid and compact molecular structure.

摘要

基于 AAZTA(6-氨基-6-甲基全氢-1,4-二氮杂环四乙酸)平台的单体和二聚体双功能螯合物,带有芳氨基和异硫氰酸酯基团,可与生物分子缀合,被合成出来。这两个系统都用于制备高弛豫率的树枝状大分子(PAMAM G1)和多聚体八-Gd(III)配合物。这些系统表现出增强的弛豫性能归因于每个金属离子上存在两个配位的、快速交换的水分子(q = 2),以及相当刚性和紧凑的分子结构。

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