Bismuth–dithiol inhibition of the Escherichia coli rho transcription termination factor

Brogan, Anita; Verghese, Jacob; Widger, William R.; Kohn, Harold

doi:10.1016/j.jinorgbio.2004.12.019

Cited by 16 publications

(10 citation statements)

References 54 publications

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“…Crystallization from absolute ethanol resulted in white crystals (50%, lit. 19 70%). The product was further recrystallized from acetone/ethanol, 1:1, v/v.…”

Section: Methodsmentioning

confidence: 99%

C4-Alkylthiols with activity against Moraxella catarrhalis and Mycobacterium tuberculosis

Kostova

Myers

Beck

et al. 2011

Bioorganic & Medicinal Chemistry

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Antimicrobial resistance represents a global threat to healthcare. The ability to adequately treat infectious diseases is increasingly under siege due to the emergence of drug-resistant microorganisms. New approaches to drug development are especially needed to target organisms that exhibit broad antibiotic resistance due to expression of β-lactamases which is the most common mechanism by which bacteria become resistant to β-lactam antibiotics. We designed and synthesized 20 novel monocyclic β-lactams with alkyl- and aryl-thio moieties at C4, and subsequently tested these for antibacterial activity. These compounds demonstrated intrinsic activity against serine β-lactamase producing Mycobacterium tuberculosis wild type strain (Mtb) and multiple (n = 6) β-lactamase producing Moraxella catarrhalis clinical isolates.

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“…Crystallization from absolute ethanol resulted in white crystals (50%, lit. 19 70%). The product was further recrystallized from acetone/ethanol, 1:1, v/v.…”

Section: Methodsmentioning

confidence: 99%

C4-Alkylthiols with activity against Moraxella catarrhalis and Mycobacterium tuberculosis

Kostova

Myers

Beck

et al. 2011

Bioorganic & Medicinal Chemistry

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“…34,45 Because of its relative simplicity, detergent sensitivity has been used in a growing number of drug discovery projects to triage compounds for promiscuity ( Table 1). 28,[34][35][36]38,39 For instance, using a library of 147 compounds derived from the Cdc25A phosphatase inhibitor dysidiolide, Koch and co-workers found selective inhibitors of three enzymes that were structurally similar to Cdc25A. All of the library compounds were assayed against each target enzyme in the presence and absence of 0.001 or 0.01% Triton X-100 to ultimately identify the specific inhibitors.…”

Section: Detergent Sensitivitymentioning

confidence: 99%

“…This assay requires that the ratio of inhibitor to enzyme remains elevated, on the order of 1000:1 or greater, even after the enzyme concentration has been increased. 13,28,36,37 For example, Disperse Blue against 3.3 mg mL À 1 phosphomannomutase/phosphoglucomutase (PMM/PGM) had an IC 50 of 5 mM; when the enzyme concentration was increased to 33 mg mL À 1 , the compound did not show any detectable inhibition up to 10 mM. In such cases, it may be helpful to decrease the initial assay concentration of the enzyme or to use alternative substrates with slower reaction rates.…”

Section: Sensitivity To Enzyme Concentrationmentioning

confidence: 99%

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Promiscuous Ligands

McGovern

2007

Comprehensive Medicinal Chemistry II

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“…Bismuth inhibits the growth of both Gram-negative and Gram-positive bacteria [5–7]. The mechanism of antimicrobial action is not completely known but involves inhibition of the Escherichia coli rho transcription termination factor [8] and iron transport [9]. More importantly, bismuth inhibits biofilm production by Staphylococci and Pseudomonas species [5,6].…”

Section: Introductionmentioning

confidence: 99%

Bismuth coating of non-tunneled haemodialysis catheters reduces bacterial colonization: a randomized controlled trial

Schindler

Heemann

Haug

et al. 2010

Nephrology Dialysis Transplantation

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Background. Haemodialysis (HD) catheter-related blood stream infections are a major cause of morbidity and mortality in patients with acute and chronic renal failure.Methods. We conducted a randomized, prospective, double-blinded trial investigating the clinical value of bismuth-coated non-tunneled HD catheters in patients in need of temporary short-term vascular access. A standard catheter (SC) was compared to a surface-modified, bismuth-film-coated catheter (FCC). After removal of the catheter for any reason, both arterial and venous lumina were rinsed and the fluid cultured for detection of bacterial colony-forming units (CFU). The catheter tip was placed in a tube containing sterile saline, sonicated and shortly centrifuged to remove debris (3 min at 1000 g). The supernatant was cultured and assayed for DNA content.Results. Seventy-seven patients in three HD units were randomized. Thirteen patients suffered from acute renal failure, 60 patients from chronic renal failure, and four patients without renal insufficiency were treated with plasma exchange. The time to catheter removal was not significantly different between groups, with a mean of 18.5 ± 2 days for SC and 15.1 ± 2 days for FCC. In most cases, the reasons for catheter removal were related to no further need for extracorporeal therapy or establishment of a permanent vascular access. Six catheters for SC and four catheters for FCC were removed because of presumed infection. Bacterial colonization was significantly lower for coated catheters compared to standard catheters, both for cultured catheter tips as well as for CFU in rinse fluids (P < 0.05).Conclusions. Surface modification with bismuth film reduces bacterial colonization of temporary non-tunneled HD catheters in a clinical trial. Larger trials with these modified catheters are justified to further investigate the effect on catheter-related infections, complications and costs.

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Bismuth–dithiol inhibition of the Escherichia coli rho transcription termination factor

Cited by 16 publications

References 54 publications

C4-Alkylthiols with activity against Moraxella catarrhalis and Mycobacterium tuberculosis

C4-Alkylthiols with activity against Moraxella catarrhalis and Mycobacterium tuberculosis

Promiscuous Ligands

Bismuth coating of non-tunneled haemodialysis catheters reduces bacterial colonization: a randomized controlled trial

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