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Application of thiazole benzamide derivatives in the preparation of anti-osteoporosis and anti-osteoarthritis drugs

A technology for benzamide and osteoarthritis, applied in the field of pharmaceutical use, can solve the problems of not being able to significantly reduce the risk of atypical fractures, failing to meet anti-osteoporosis treatment, failing to meet treatment needs, etc., achieving novel structure, Simple structure and low toxicity

Active Publication Date: 2021-12-24
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the above-mentioned drugs can prevent the decline of bone mineral density to a certain extent, they cannot significantly reduce the risk of atypical fractures, and there are side effects of varying degrees, which have not yet met the requirements of anti-osteoporosis treatment (Siris, Selby et al. al.2009)
Therefore, there is an urgent need to develop a new anti-osteoporosis specific drug to solve the problem that the current clinical drugs cannot meet the treatment needs.

Method used

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  • Application of thiazole benzamide derivatives in the preparation of anti-osteoporosis and anti-osteoarthritis drugs
  • Application of thiazole benzamide derivatives in the preparation of anti-osteoporosis and anti-osteoarthritis drugs
  • Application of thiazole benzamide derivatives in the preparation of anti-osteoporosis and anti-osteoarthritis drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: synthesis of thiazole benzamide derivatives

[0047]

Embodiment 2

[0048] Example 2: NF-κB signaling pathway inhibition experiment

[0049] S1. Cell culture.

[0050]RAW264.7 cells stably transfected with high expression of NF-κB were cultured in vitro. DMEM high-glucose medium containing 10% fetal bovine serum was used for routine maintenance and passage at 37°C and 5% carbon dioxide concentration.

[0051] S2. Compound intervention.

[0052] Collect logarithmic phase cells and make the cell suspension concentration 5×10 5 cells / ml, added to 96-well cell culture plate. After culturing in a carbon dioxide incubator for 24 hours, the culture medium was replaced with media containing different compound concentrations, and co-cultivated for 6 hours. The compounds to be tested were prepared as solutions at different concentrations using DMSO. Three parallel wells were set up for each concentration, and a control group without compound treatment was set up for comparison.

[0053] S3. Test method.

[0054] After the experiment, the cells we...

Embodiment 3

[0059] Example 3: Toxicity assay of compound cells

[0060] S1. Cell culture.

[0061] RAW264.7 cells were cultured in vitro. DMEM high-glucose medium containing 10% fetal bovine serum was used for routine maintenance and passage at 37°C and 5% carbon dioxide concentration.

[0062] S2. Compound intervention.

[0063] Collect logarithmic phase cells and make the cell suspension concentration 1×10 5 cells / ml, added to 96-well cell culture plate. After culturing in a carbon dioxide incubator for 24 hours, the culture solution was replaced with a medium containing different compound concentrations, and the culture was continued for 2 days, and the cytotoxicity was detected on the 3rd day. The compounds to be tested were prepared as solutions at different concentrations using DMSO. Three parallel wells were set up for each concentration, and a control group without compound treatment was set up for comparison.

[0064] S3. Test method.

[0065] MTT [3-(4,5-dimethylthiazole-...

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PUM

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Abstract

The invention discloses the application of thiazole benzamide derivatives as osteoclast differentiation inhibitors in the preparation of anti-osteoporosis drugs. The structural formula of the thiazole benzamide derivative is shown in formula (I). The thiazole amide derivatives provided by the present invention are different from the molecular skeletons of osteoporosis prevention and treatment drugs currently used clinically such as phosphates, estrogen drugs, and parathyroid hormone inhibitors, and have high osteoclast differentiation inhibitory activity, Little toxicity. Therefore, this compound can be used as a new type of compound for preventing and treating related diseases caused by abnormal differentiation of osteoclasts, especially osteoporosis or osteopenia.

Description

technical field [0001] The present invention relates to the technical field of drug application, more specifically, relates to the application of thiazole benzamide derivatives in the preparation of anti-osteoporosis and anti-osteoarthritis drugs. Background technique [0002] Osteoporosis and osteoarthritis are common orthopedic diseases. Osteoporosis is a skeletal disease characterized by increased bone fragility and fracture risk due to decreased bone mass and microarchitectural degradation of bone tissue. With the aging of our society, the incidence of this disease is increasing year by year. Epidemiological research shows that among people over 50 years old, about 50% of women and 20% of men are at risk of fracture (Rachner, Khosla et al. 2011). According to the data of the National Bureau of Statistics: by 2050, the population over 50 years old in my country will be nearly half (49%) of the national population, about 636 million. It is estimated that by 2050, the num...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/625A61K31/426A61K31/428A61K31/427A61K31/4402A61P19/02A61P19/10C07D277/46C07D277/56C07D277/82C07D417/12C07D213/75
CPCC07D277/46C07D277/56C07D277/82C07D417/12A61P19/10
Inventor 顾琼徐峻黄丹娥赵超
Owner SUN YAT SEN UNIV
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