Semi-synthetic aminoglycoside antibiotic, preparation method and medicine composition thereof

An aminoglycoside and semi-synthetic technology, which is applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., can solve the problems of high production costs, and achieve the effects of high application value, high yield and pure products
CN102321131AInactive Publication Date: 2012-01-18CHANGZHOU FANGYUAN PHARMA
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Applications(China)
Current Assignee / Owner
CHANGZHOU FANGYUAN PHARMA
Publication Date
2012-01-18
Estimated Expiration
Not applicable Β· inactive patent

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Abstract

The invention discloses a semi-synthetic aminoglycoside antibiotic of 1-N-acetyl micronomicin, and pharmaceutically acceptable salt and a preparation method thereof. The preparation method of 1-N-acetyl micronomicin comprises the following steps: the formylation protection is carried out on C2'-NH2 and C3-NH2 of micronomicin basic groups, the 3,-2-two-N-formoxyl micronomicin, the acetylation reaction is then carried out to obtain 1-N-acetyl-3,-2-two-N-formoxyl micronomicin, the obtained products are subject to hydrolysis reaction in alkali solution, and the 1-N-acetyl micronomicin is obtained through formylation protection for removing 2'-NH2 and 3-NH2. The 1-N-acetyl micronomicin has the advantages that in-vitro antitubercular bacteria and antibiotic activity experiments prove that the 1-N-acetyl micronomicin has higher antibiotic activity to mycobacterium tuberculosis gram-positive bacteria and negative bacteria, in addition, the toxicity of medicine on ears and kidneys is greatly reduced, and higher clinical application value is realized.
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Description

technical field

[0001] The present invention relates to an aminoglycoside antibiotic, in particular to a new antibacterial compound 1-N-acetyl agnonomycin or its salt, its preparation method and a pharmaceutical composition containing the active ingredient. Background technique

[0002] Since the American scholar Waxman discovered the first aminoglycoside antibiotic streptomycin (streptomycin) in 1944, after more than 60 years of development, this type of antibiotic has been widely used in the treatment of anti-infective diseases. Aminoglycoside antibiotics not only have a broad antibacterial spectrum, but also do not have fatal allergic reactions like penicillin. When aminoglycoside antibiotics are used in combination with Ξ²-lactam antibiotics, they have a better synergistic effect on severe patients. However, due to the side effects of certain ear and kidney aspects of these antibiotics, their widespread clinical use is limited. After the long-term efforts of scholars, ma...

Claims

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