AI Article Synopsis
- - New antibacterial compounds called 3-(aminothiazolyl)quinolones (ATQs) were developed to fight increasing drug resistance in animals during farming.
- - Two specific ATQs, ,-dicyclohexylaminocarbonyl ATQ and methyl ATQ, demonstrated superior antibacterial activity compared to the traditional drug norfloxacin, with lower toxicity to mammalian cells.
- - ATQs work by disrupting bacterial biofilms, damaging bacterial membranes, binding to DNA to prevent replication, and generating reactive oxygen species, making them promising candidates for treating animal bacterial infections.
Article Abstract
New antibacterial 3-(aminothiazolyl)quinolones (ATQs) were designed and efficiently synthesized to counteract the growing multidrug resistance in animal husbandry. Bioactive assays manifested that ,-dicyclohexylaminocarbonyl ATQ and methyl ATQ , respectively, showed better antibacterial behavior against ATCC 29213 and than reference drug norfloxacin. Notably, highly active ATQ with low hemolysis, negligible mammalian cytotoxicity, and good pharmacokinetic properties displayed low trends to induce resistance and synergistic combinations with norfloxacin. Preliminary mechanism exploration implied that representative ATQ could inhibit the formation of biofilms and destroy bacterial membrane integrity, further binding to intracellular DNA and DNA gyrase to hinder bacterial DNA replication. ATQ could also induce the production of excess reactive oxygen species and reduce bacterial metabolism to accelerate bacterial death. These results provided a promise for 3-(aminothiazolyl)quinolones as new potential multitargeting antibacterial agents to treat bacterial infection of animals.
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| http://dx.doi.org/10.1021/acs.jafc.2c08293 | DOI Listing |
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