AI Article Synopsis
- - A new series of pleuromutilin derivatives were created and found to be effective against various strains of drug-resistant bacteria, including MRSA and MSSA.
- - One compound showed exceptional antibacterial effectiveness in lab tests, with minimal side effects and a low chance of fostering bacterial resistance.
- - In animal studies, this compound successfully reduced MRSA infections and improved healing by lowering inflammation, indicating its potential as a treatment for resistant bacterial infections.
Article Abstract
A series of pleuromutilin derivatives containing an oxazolidinone skeleton were synthesized and evaluated in vitro and in vivo as antibacterial agents. Most of the synthesized derivatives exhibited potent antibacterial activities against three strains of (including MRSA ATCC 33591, MRSA ATCC 43300, and MSSA ATCC 29213) and two strains of (including MRSE ATCC 51625 and MSSE ATCC 12228). Compound was the most active antibacterial agent in vitro (MIC = 0.008-0.125 μg·mL) and exhibited a significant bactericidal effect, low cytotoxicity, and weak inhibition (IC = 20.66 μmol·L) for CYP3A4, as well as exhibited less possibility to cause bacterial resistance. Furthermore, in vivo activities indicated that the compound was effective in reducing MRSA load in a murine thigh infection model. Moreover, it clearly facilitated the healing of MRSA skin infection and inhibited the secretion of the TNF-α, IL-6, and MCP-1 inflammatory factors in serum. These results suggest that oxazolidinone pleuromutilin is a promising therapeutic candidate for drug-resistant bacterial infections.
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| http://dx.doi.org/10.1021/acsinfecdis.3c00162 | DOI Listing |
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