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Chemical Structure| 1261444-00-1 Chemical Structure| 1261444-00-1

Structure of 1261444-00-1

Chemical Structure| 1261444-00-1

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Zore, Matej ; San-Martin-Galindo, Paola ; Reigada, Ines ; Hanski, Leena ; Fallarero, Adyary ; Yli-Kauhaluoma, Jari , et al.

Abstract: The emergence of multidrug-resistant bacteria along with a declining pipeline of clinically useful antibiotics has led to the urgent need for the development of more effective agents. Inspired by our recent report on the activity of , an immunomodulating drug candidate, we prepared a series of derivatives by varying substituents on the phenyl ring, altering the central tricyclic aromatic ring, and modifying the carboxyl group. From this series of compounds, derivative 24f was identified as the most potent compound, with the minimum inhibitory concentration (MIC) values between 2.5 and 10 μM against various Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), S. epidermidis and enterococci. Moreover, 24f exhibited rapid bactericidal activity against S. aureus, low toxicity and hemolytic activity, and a synergistic effect with gentamicin against S. aureus, MRSA, and Enterococcus faecalis. Furthermore, it was shown that neither nor 24f affects S. aureus cell membranes. Importantly, 24f did not induce resistance in S. aureus, representing a significant improvement compared to . Finally, the activity of and 24f against S. aureus and MRSA was confirmed in vivo in a Caenorhabditis elegans infection model. Taken together, our study highlights the value of and its derivatives as potential candidates for combating infections caused by Gram-positive bacteria.

Keywords: activity ; Derivatives ; ; MRSA ; Staphylococcus aureus

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Product Details of [ 1261444-00-1 ]

CAS No. :1261444-00-1
Formula : C9H6ClF3O3
M.W : 254.59
SMILES Code : O=C(OC)C1=CC=C(Cl)C(OC(F)(F)F)=C1
MDL No. :MFCD18399027

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