In a mouse model of abdominal infection, ZJ-2 decreased the bacterial load and the level of IL-6 and TNF-α in a time-dependent manner. Moreover, ZJ-2 can be docked into SagA to inhibit daughter cell separation. Diarylurea ZJ-2 with benign drug-like property exhibited potent antibacterial and anti-biofilm activity through inhibiting the genes expression of NlpC/p60 hydrolase-secreted antigen A (sagA) and autolysins (atlA), down-regulating the expression of biofilm adherence related genes aggregation substance (agg), enterococcal surface protein (esp) against E. In this study, the diarylurea scaffold was found to have potent antibacterial effect on E. faecium) is a clinical multidrug-resistant pathogen causing life-threatening infection, which makes it important to discover antibacterial agents with novel scaffolds and unique mechanism. Overall, our data showed that the aromatic hydrazone is a promising scaffold for anti-staphylococcal drug development.Įnterococcus faecium (E. MTT assay showed that compound 2e displays as low toxicity as CCCP. Moreover, electron microscopy revealed that compound 2e inhibits biofilm formation and effectively eradicates preformed biofilm. In particular, when compound 2e is combined with ofloxacin, it has a good synergistic effect against MRSA. Some compounds in combination with antibiotics exhibited potentiate Gram-positive antibacterial activity compound 2e was found to display unaided or synergistic efficacy against MRSA. aureus and methicillin resistant Staphylococcus aureus (1.56 and 1.56 μM, respectively). To improve CCCP's potency and toxicity, a series of aromatic hydrazones were synthesized and their antimicrobial activity was evaluated amongst them, compounds 2e and 2j with a strong para-electron-withdrawing substituent (–NO2 and –CF3) at the phenyl ring had the lowest MICs against both S. Carbonyl cyanide m-chlorophenylhydrazone (CCCP), as a protonophore, in combination with antibiotics exhibited potentiating antibacterial activity.
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