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Technetium-99m-labeled isonitrile-containing UBI 29-41 derivative as well as preparation method and application thereof

A derivative and labeling technology, which is applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of low target-to-non-target ratio and uncertain structure of markers, and achieves simple preparation, good stability, and good inflammation/muscle ratio Effect

Active Publication Date: 2022-03-25
BEIJING NORMAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Technetium-99m-labeled antibacterial peptide (99mTc-UBI 29-41) has been used clinically as a radiopharmaceutical for the diagnosis of bacterial inflammation. It can distinguish bacterial inflammation from non-bacterial inflammation, but its There are still some deficiencies such as uncertain marker structure and low ratio of target to non-target, so it is necessary to develop a new type of bacterial inflammation imaging agent

Method used

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  • Technetium-99m-labeled isonitrile-containing UBI 29-41 derivative as well as preparation method and application thereof
  • Technetium-99m-labeled isonitrile-containing UBI 29-41 derivative as well as preparation method and application thereof
  • Technetium-99m-labeled isonitrile-containing UBI 29-41 derivative as well as preparation method and application thereof

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Embodiment Construction

[0041] Describe the present invention in detail below by embodiment: a kind of 99m Tc-CNUBI 29-41 complex, its structural formula is as follows:

[0042]

[0043] In the structural formula: with 99m Tc + The core is the central core, and the carbon atom of the isonitrile in the ligand molecule of CNUBI 29-41 and 99m Tc coordinates to form a hexacoordinated 99m Tc-CNUBI 29-41 complex. However, n represents an integer of 2 or more.

[0044] a. Synthesis of ligand CNUBI 29-41:

[0045] Weigh an appropriate amount of triethylamine into a round bottom flask, add an appropriate amount of N,N-dimethylformamide to dissolve, then add an appropriate amount of UBI 29-41, and dropwise add dichloromethane containing 1.2 times the equivalent of compound 1 (n=5) Solution, overnight reaction at room temperature, after the reaction, preparative HPLC (mobile phase: A phase is water, B phase is acetonitrile, flow rate is 10mL / min. Elution gradient: 0-20min, 10%-99%B; 20 -30min, 99%B; 3...

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Abstract

The invention discloses a < 99m > Tc-labeled isonitrile-containing UBI 29-41 derivative and a preparation method and application thereof.The < 99m > Tc-labeled isonitrile-containing UBI 29-41 derivative is characterized in that an antibacterial peptide fragment UBI 29-41 with bacterial specificity is converted into an isonitrile-based antibacterial peptide ligand (CNUBI 29-41) capable of being complexed with < 99m > Tc, and a < 99m > Tc-CNUBI 29-41 complex is obtained through a preparation process that isonitrile in the CNUBI 29-41 ligand is coordinated with < 99m > Tc. The complex is a hydrophilic substance, is high in radiochemical purity, good in stability, simple and convenient to prepare, high in uptake and good in retention at bacterial inflammation parts, good in inflammation / muscle ratio, capable of distinguishing bacterial inflammation and non-bacterial inflammation, and capable of serving as a novel bacterial inflammation imaging agent to be popularized and applied.

Description

Technical field: [0001] The invention relates to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a technetium-99m-labeled isonitrile-containing UBI 29-41 derivative, a preparation method and application. Background technique: [0002] Inflammation is a common and important pathological process, and the inflammatory response is closely related to human health. Although the emergence of antibiotics has greatly improved the treatment of inflammation, with the development of modern medicine, the use of various chemotherapeutic agents, instrument implantation and surgical operations such as organ transplantation have resulted in more and more patients with low immunity. In addition, the extensive use of antibiotics has also reduced the sensitivity of the body to these drugs. The global abuse of antibiotics has made bacteria more resistant to drugs, and even superbugs have emerged. Today, inflammation is still one of the most ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08C07K7/08C07K1/13A61K103/10
CPCA61K51/08C07K7/08
Inventor 张俊波江雨豪冯俊红阮晴王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY