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Novel Carbohydrate-Appended Metal Complexes for Potential Use in Molecular Imaging

机译:可能在分子成像中使用的新型碳水化合物金属配合物

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Seven discrete sugar-pendant diamines were complexed to the JM(CO)3}+(99nTc/Re)core:1,3-diami-no-2-propyl p-D-glucopyranoside(L1),1,3-diamino-2-propyl fi-D-xylopyrano-side(L2),l,3-diamino-2-propyl a-D-mannopyranoside(L3),l,3-diamino-2-propyl a-o-galactopyranoside(L4),1,3-diamino-2-propyl(3-D-galactopyrano-side(L5),l,3-diamino-2-propyl(3-(a-D-glucopyranosyl-(l,4)-D-glucopyrano-side)(L6),and bis(aminomethyl)bis[(p-D-glucopyranosyloxy)methyl]methane(L7).The Re complexes[Re(L1-L7)(Br)(CO)3]were characterized by 'H and 13C 1D/2D NMR spectroscopy which confirmed the pendant nature of the carbohydrate moieties in solution.Additional characterization was provided by IR spectroscopy,elemental analysis,and mass spectrometry.Two analogues,[Re(L2)(CO)3Br]and[Re-(L3)(CO)3Br],were characterized in the solid state by X-ray crystallography and represent the first reported structures of Re organometallic carbohydrate compounds.Conductivity measurements in H_2O established that the complexes exist as[Re(L'-L7)-(H_2O)(CO)JBr in aqueous conditions.Radiolabelling of L'-L7 with[99mTc(H_20)3(CO)3]+ afforded in high yield compounds of identical character to the Re analogues.The radiolabelled compounds were determined to exhibit high in vitro stability towards ligand exchange in the presence of an excess of either cysteine or histidine over a 24 h period.
机译:七个离散的糖链二胺与JM(CO)3} +(99nTc / Re)核心复合:1,3-二氨基-无-2-丙基pD-吡喃葡萄糖苷(L1),1,3-二氨基-2-丙基FI-D-吡喃并吡喃糖苷(L2),1,3-二氨基-2-丙基aD-甘露吡喃糖苷(L3),1,3-二氨基-2-丙基拟吡喃半乳糖苷(L4),1,3-二氨基- 2-丙基(3-D-吡喃半乳糖侧(L5),1,3-二氨基-2-丙基(3-(aD-吡喃吡喃糖基-(l,4)-D-吡喃吡喃侧)(L6)和bis (氨基甲基)双[(pD-吡喃葡萄糖基氧基)甲基]甲烷(L7)。Re配合物[Re(L1-L7)(Br)(CO)3]的特征在于'H和13C 1D / 2D NMR谱图,证实了溶液中碳水化合物部分的侧基性质。通过红外光谱,元素分析和质谱法进行了表征。[Re(L2)(CO)3Br]和[Re-(L3)(CO)3Br]的两个类似物,在X射线晶体学上表征为固态,并代表了最早报道的Re有机金属碳水化合物化合物的结构。在H_2O中的电导率测量表明,络合物以[Re (L'-L7)-(H_2O)(CO)JBr在水性条件下。用[99mTc(H_20)3(CO)3] +对L'-L7进行放射提振,可制得具有与Re类似物相同性质的高产率化合物。确定在24小时内存在过量半胱氨酸或组氨酸的情况下,放射性标记的化合物对配体交换具有很高的体外稳定性。

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