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Trimolecular conjugate taking p-aminosalicylic acid as mother nucleus, intermediate, preparation method and application

A technology of p-aminosalicylic acid and conjugates, which is applied in the directions of medical preparations without active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas

Active Publication Date: 2022-05-13
SOUTHWEST UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Multi-target drug design strategy is a new idea to solve complex diseases, especially multi-target diseases

Method used

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  • Trimolecular conjugate taking p-aminosalicylic acid as mother nucleus, intermediate, preparation method and application
  • Trimolecular conjugate taking p-aminosalicylic acid as mother nucleus, intermediate, preparation method and application
  • Trimolecular conjugate taking p-aminosalicylic acid as mother nucleus, intermediate, preparation method and application

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Embodiment Construction

[0047] In order to make the object, technical solution and beneficial effect of the present invention clearer, preferred embodiments of the present invention will be described in detail below.

[0048] Main chemical reagents and instruments

[0049] PAS (Shanghai Titan Co., Ltd., 98%); INA, concentrated sulfuric acid, methanol, ethanol, sodium bicarbonate, potassium carbonate (Chongqing Chuandong Chemical Co., Ltd.); Clinfloxacin (CLX), Ciprofloxacin (CIP), salad Floxacin (SAR), Enoxacin (ENX), Baloxacin (BAL), Gatifloxacin (GAT) (Zhengzhou Keertai Biochemical Technology Co., Ltd., >95%); Norfloxacin (NOR ), lomefloxacin (LOM) (Shanghai Darui Fine Chemical Co., Ltd., AR); chloroacetyl chloride, 3-chloropropionyl chloride (Chongqing Tixin Chemical Co., Ltd.); the rest of the reagents are commercially available chemically pure or analytically pure products , used directly without purification.

[0050] Nuclear Magnetic Resonance (Bruker, ADVANCEⅢ TM 600 MHz, TMS as internal ...

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Abstract

The invention discloses a trimolecular conjugate taking p-aminosalicylic acid (PAS) as a mother nucleus, which is shown in a formula I, wherein the trimolecular conjugate is formed by conjugating three structural units, namely PAS, isonicotinic acid and fluoroquinolone; anti-human pathogenic bacterium activity tests prove that the trimolecular conjugate synthesized by the invention has certain antibacterial activity, especially has a plurality of molecules with high antibacterial activity on mycobacterium tuberculosis, salmonella, pseudomonas aeruginosa and staphylococcus aureus, and meanwhile, hemolytic tests verify the safety of the molecules, so that the trimolecular conjugate can be used for preparing the antibacterial peptide. The polypeptide has the potential of further developing and researching antibacterial drugs, especially antituberculosis drugs.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and relates to a trimolecular conjugate with p-aminosalicylic acid (PAS) as a mother nucleus, an intermediate, a preparation method and a pharmaceutical application. Background technique [0002] Tuberculosis (Tuberculosis, TB) is a chronic fatal infectious disease caused by Mycobacterium tuberculosis (MTB). Before the coronavirus (COVID-19) pandemic, tuberculosis was the leading cause of death from a single infectious disease, ranking higher than AIDS. Today, TB remains a global public health problem. [0003] The World Health Organization (WHO) divides anti-tuberculosis drugs into first-line and second-line anti-tuberculosis drugs according to their effects and side effects. First-line TB drugs streptomycin (Streptomycin, SM), isoniazid (INH, H), pyrazinamide (PZA, Z), rifampicin (RIF, R) and ethambutol ( Ethambutol, EMB, E) have significant curative effect, less side effects, and can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14C07D401/12C07D471/04C07D213/79C07D213/803A61K31/618A61K31/4409A61K31/4709A61K31/496A61K31/625A61K47/55A61P31/04A61P31/06
CPCC07D401/14C07D401/12C07D471/04C07D213/79C07D213/803A61K31/618A61K31/4409A61K31/4709A61K31/496A61K31/625A61K47/552A61P31/04A61P31/06Y02A50/30
Inventor 范莉杨大成任艳会谢建平许峻旗代乐平毛丹杨茜周成合
Owner SOUTHWEST UNIVERSITY
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