Preparation method and application of deuterated drugs

A technology of deuterium and medicine, applied in the field of medicine and medicine, can solve the problems of limited technical approaches and means of chemical bonds and hydrogen bond energy

Inactive Publication Date: 2011-04-20
陈松源
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, the technical approaches and means to change the chemical bonds and h...

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  • Preparation method and application of deuterated drugs
  • Preparation method and application of deuterated drugs
  • Preparation method and application of deuterated drugs

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Embodiment Construction

[0034] 1. Preparation of deuterated isoniazid:

[0035] Isoniazid was once a widely used anti-tuberculosis drug, which has a bactericidal effect on Mycobacterium tuberculosis, and Mycobacterium tuberculosis is prone to develop drug resistance to this product. Since the current clinical tuberculosis pathogenic strains are mainly drug-resistant strains, isoniazid is no longer used alone, but in combination with other anti-tuberculosis drugs. Large doses of isoniazid can easily cause liver damage, and combined use of rifampicin can significantly increase liver damage. Therefore, increasing the sensitivity of isoniazid to Mycobacterium tuberculosis and reducing the dosage has obvious clinical value. Therefore, Isoniazid was selected for deuterium substitution to develop new anti-tuberculosis drugs.

[0036] Chinese name: Isoniazid;

[0037] English name: Isoniazid;

[0038] Chemical name: 4-pyridinecarbohydrazide

[0039] CAS NO: 54-85-3

[0040] Molecular formula: C 6 h 7...

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Abstract

A carbon hydrogen structure (C: H) is one of the basic structures in the pharmaceutical chemistry structure and a formed C-H bond is the basic chemical bond. The invention discloses a preparation method and an application of deuterated drugs which can change the chemical bond energy and the hydrogen bond energy in the structure of pharmaceutical compound. The hydrogen atom (H) in pharmaceutical compound structure is substituted by the A deuterium atom (D) which is the isotope of hydrogen, therefore changing the molecular structure and the bond energy of the substituted pharmaceutical compound so as to form a new deuterated drug. The deuterated drugs can be used for pharmacokinetics research, can obviously enhance the disease-preventing or treating function of the drugs, and can reduce the toxic and side effect of the drugs.

Description

technical field [0001] The invention belongs to the technical field of medical medicine, in particular to a preparation method and application of deuterated medicine. Background technique [0002] In the molecular structure of pharmaceutical compounds, the carbon:hydrogen structure (C:H) is the most basic structure, and the formed carbon-hydrogen bond (C-H) is also the most basic chemical bond. The hydrogen bond is represented by X-H...Y, and the distance between X-Y It is defined as the bond length of the hydrogen bond. The hydrogen bond has bond energy. The structural parameters of the hydrogen bond such as bond length, bond angle, and squareness can vary in a considerable range and affect the bond energy. The shorter the bond length, the stronger the hydrogen bond . Although the bond energy of hydrogen bonds is not large, it has a great impact on the properties of substances. There are two reasons: 1. The principle of forming the most hydrogen bonds, the substance tends ...

Claims

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Application Information

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IPC IPC(8): C07B59/00C07D213/86C07D417/12A61K31/4409A61P31/06A61K31/4439A61P3/10
Inventor 不公告发明人
Owner 陈松源
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