Synthesis and anti-biofilm activity of thiazole Schiff bases

More, P. G.; Karale, Netaji N.; Lawand, A. S.; Narang, Naina; Patil, Rajendra

doi:10.1007/s00044-013-0672-7

Cited by 34 publications

(21 citation statements)

References 47 publications

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“…Recent studies have demonstrated that thiazole and thiazolidinone compounds possess the ability to disrupt bacterial biofilms 38,39 . To examine if the potential therapeutic application of 1 and 2 could be expanded beyond just inhibition of planktonic bacteria, the ability of both thiazole compounds to disrupt staphylococcal biofilm was analyzed.…”

Section: Resultsmentioning

confidence: 99%

Anti-biofilm activity and synergism of novel thiazole compounds with glycopeptide antibiotics against multidrug-resistant Staphylococci

et al. 2014

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Methicillin-resistant Staphylococcus aureus (MRSA) infections are a leading cause of death among all fatalities caused by antibiotic-resistant bacteria. With the rise of increasing resistance to current antibiotics, new antimicrobials and treatment strategies are urgently needed. Thiazole compounds have been shown to possess potent antimicrobial activity. A lead thiazole 1 and a potent derivative 2 were synthesized and their activity in combination with glycopeptide antibiotics was determined against an array of MRSA and vancomycin-resistant Staphylococcus aureus (VRSA) clinical isolates. Additionally, the anti-biofilm activity of the novel thiazoles was investigated against Staphylococcus epidermidis. Compound 2 behaved synergistically with vancomycin against MRSA and was able to re-sensitize VRSA to vancomycin, reducing its minimum inhibitory concentration (MIC) by 512-fold in two strains. Additionally, both thiazole compounds were superior to vancomycin in significantly reducing S. epidermidis biofilm mass. Collectively the results obtained demonstrate compounds 1 and 2 possess potent antimicrobial activity alone or in combination with vancomycin against multidrug-resistant staphylococci and show potential for use in disrupting staphylococcal biofilm.

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Section: Resultsmentioning

confidence: 99%

Anti-biofilm activity and synergism of novel thiazole compounds with glycopeptide antibiotics against multidrug-resistant Staphylococci

et al. 2014

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“…Because QS is involved in microbial pathogenesis, chemicals that inhibit QS have been developed to control bacterial diseases. Some thiazole compounds have substantial anti-biofilm activity in Gram-positive and Gram-negative bacteria (Mohammad et al, 2015;More et al, 2014;Rane et al, 2012). Some 1,3,4-thiadiazole derivatives demonstrate good anti-QS activity in Gramnegative bacteria (El-Gohary and Shaaban, 2013.…”

Section: Discussionmentioning

confidence: 99%

A thiadiazole reduces the virulence of Xanthomonas oryzae pv. oryzae by inhibiting the histidine utilization pathway and quorum sensing

Liang

Pan

et al. 2016

Molecular Plant Pathology

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Thiazole, isothiazole, thiadiazole and their derivatives are widely thought to induce host defences against plant pathogens. In this article, we report that bismerthiazol, a thiadiazole molecule, reduces disease by inhibiting the histidine utilization (Hut) pathway and quorum sensing (QS). Bismerthiazol provides excellent control of bacterial rice leaf blight (BLB) caused by Xanthomonas oryzae pv. oryzae (Xoo), but does not greatly inhibit Xoo growth in vitro. According to RNA-sequencing analysis, the transcription of the Hut pathway genes of Xoo ZJ173 was inhibited after 4.5 and 9.0 h of bismerthiazol treatment. Functional studies of hutG and hutU indicated that the Hut pathway had little effect on the growth and bismerthiazol sensitivity of Xoo in vitro, but significantly reduced the aggregation of Xoo cells. Deletion mutants of hutG or hutU were more motile, produced less biofilm and were less virulent than the wild-type, indicating that the Hut pathway is involved in QS and contributes to virulence. The overexpression of the hutG-U operons in ZJ173 reduced Xoo control by bismerthiazol. Bismerthiazol did not inhibit the transcription of Hut pathway genes, QS or virulence of the bismerthiazol-resistant strain 2-1-1. The results indicate that bismerthiazol reduces Xoo virulence by inhibiting the Hut pathway and QS.

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“…[39] Combiningt he 4-(2-fluorophenyl)morpholinyl group and Schiff base together,S angshetti et al synthesized as eries of linezolid-like Schiff bases as antibacterial agents. [39] Combiningt he 4-(2-fluorophenyl)morpholinyl group and Schiff base together,S angshetti et al synthesized as eries of linezolid-like Schiff bases as antibacterial agents.…”

Section: Othersmentioning

confidence: 99%

“…More et al reported thiazole Schiff bases as biofilm inhibitors of P. aeruginosa. [39] ChemMedChem 2017, 12,420 -425 www.chemmedchem.org agents. [40] In particular,c ompounds 30 and 31 exhibitedg ood biofilm inhibitory activity,w ith respective IC 50 values of 12.9 and 15.6 mm against P. aeruginosa,m ore active than standard linezolid.…”

Section: Othersmentioning

confidence: 99%

Recent Advances in the Discovery of PqsD Inhibitors as Antimicrobial Agents

Zhou

2017

ChemMedChem

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The treatment of the infections caused by Pseudomonas aeruginosa, an opportunistic Gram-negative bacterium, is very difficult. High intrinsic tolerance toward common antibiotics and the development of new resistant strains challenge us to find a new treatment as soon as possible. PqsD is an enzyme essential for the P. aeruginosa quorum-sensing apparatus, which catalyzes the final and key step in the biosynthesis of 4-hydroxy-2-heptylquinolone (HHQ), which is a signal molecule of the P. aeruginosa quorum-sensing system. In this review, following an outline on their structures, we present a brief introduction of the PqsD inhibitors including their mechanisms of action, inhibitory activity, and structure-activity relationships.

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Synthesis and anti-biofilm activity of thiazole Schiff bases

Cited by 34 publications

References 47 publications

Anti-biofilm activity and synergism of novel thiazole compounds with glycopeptide antibiotics against multidrug-resistant Staphylococci

Anti-biofilm activity and synergism of novel thiazole compounds with glycopeptide antibiotics against multidrug-resistant Staphylococci

A thiadiazole reduces the virulence of Xanthomonas oryzae pv. oryzae by inhibiting the histidine utilization pathway and quorum sensing

Recent Advances in the Discovery of PqsD Inhibitors as Antimicrobial Agents

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