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Nowadays, the problem of bacterial resistance caused by the abuse of antibiotics is becoming a public health issue of increasing concern around the world.
In addition to calling on all sectors of society to use antibiotics rationally, the development of new antibiotics to overcome bacterial resistance has also become a problem that scientists need to overcome
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Nowadays, the problem of bacterial resistance caused by the abuse of antibiotics is becoming a public health issue of increasing concern around the world.
For 50 years, the search and development of antibiotics has always relied on the semi-synthetic chemical modification of natural products.
However, this method is no longer able to cope with the rapidly evolving bacterial resistance threat, and the fully synthetic chemical modification will be able to easily be designed with reasonable design.
DOI : https://doi.
org/10.
DOI : https://doi.
In this study, the researchers used the lincosamide antibiotic clindamycin as the research object to synthesize a new antibiotic
The researchers first generated 500 antibiotic drug candidates based on the combination of no chemical bonds .
After a series of tests, they selected one of the more active antibiotics and named it iboxamycin ( IBX )
Subsequently, the researchers used standard strains of Streptococcus pyogenes and methicillin-resistant Staphylococcus aureus to study the activity of IBX in mice.
The results showed that IBX achieved a statistically significant reduction in bacterial load 12 hours after treatment of mice.
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In the systemic infection model, IBX is well tolerated and safe at all dose levels .
At the same time, X -ray imaging results show that iboxamycin can shift methylated ribosomal nucleotides, exposing the drug binding site, so that the drug can still bind to and overcome the ribosome when the ribosome has been methylated.
Figure: Antibacterial activity of broad-spectrum antibiotic IBX in vitro and in vivo in mice
Figure: Antibacterial activity of broad-spectrum antibiotic IBX in vitro and in vivo in miceThe researchers said that this discovery proves the importance of synthetic chemistry and is more helpful in the development of synthetic antibiotics against drug-resistant bacteria
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Reference materials:
[1]https://#citeas
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