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排序方式: 共有1177条查询结果,搜索用时 15 毫秒
1.
Jennie O'Loughlin Silvia Napolitano Fahad Alkhathami Cillian O'Beirne Daniel Marhöfer Megan O'Shaughnessy Prof. Orla Howe Prof. Matthias Tacke Dr. Marina Rubini 《Chembiochem : a European journal of chemical biology》2021,22(6):1093-1098
Antibiotic resistance is a growing problem for public health and associated with increasing economic costs and mortality rates. Silver and silver-related compounds have been used for centuries due to their antimicrobial properties. In this work, we show that 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene silver(I) acetate/NHC*-Ag-OAc (SBC3) is a reversible, high affinity inhibitor of E. coli thioredoxin reductase (TrxR; Ki=10.8±1.2 nM). Minimal inhibition concentration (MIC) tests with different E. coli and P. aeruginosa strains demonstrated that SBC3 can efficiently inhibit bacterial cell growth, especially in combination with established antibiotics like gentamicin. Our results show that SBC3 is a promising antibiotic drug candidate targeting bacterial TrxR. 相似文献
2.
Bram H. Frohock Jessica M. Gilbertie Dr. Jennifer C. Daiker Dr. Lauren V. Schnabel Dr. Joshua G. Pierce 《Chembiochem : a European journal of chemical biology》2020,21(7):933-937
The failure of frontline antibiotics in the clinic is one of the most serious threats to human health and requires a multitude of novel therapeutics and innovative approaches to treatment so as to curtail the growing crisis. In addition to traditional resistance mechanisms resulting in the lack of efficacy of many antibiotics, most chronic and recurring infections are further made tolerant to antibiotic action by the presence of biofilms. Herein, we report an expanded set of 5-benzylidene-4-oxazolidinones that are able to inhibit the formation of Staphylococcus aureus biofilms, disperse preformed biofilms, and, in combination with common antibiotics, are able to significantly reduce the bacterial load in a robust collagen-matrix model of biofilm infection. 相似文献
3.
Dr. Emilianne M. Limbrick Audrey E. Yñigez-Gutierrez Callie C. Dulin Dagmara K. Derewacz Dr. Jeffrey M. Spraggins Dr. Kathryn M. McCulloch Prof. T. M. Iverson Prof. Brian O. Bachmann 《Chembiochem : a European journal of chemical biology》2020,21(23):3349-3358
Everninomicins are orthoester oligosaccharide antibiotics with potent activity against multidrug-resistant bacterial pathogens. Everninomicins act by disrupting ribosomal assembly in a distinct region in comparison to clinically prescribed drugs. We employed microporous intergeneric conjugation with Escherichia coli to manipulate Micromonospora for targeted gene-replacement studies of multiple putative methyltransferases across the octasaccharide scaffold of everninomicin effecting the A1, C, F, and H rings. Analyses of gene-replacement and genetic complementation mutants established the mutability of the everninomicin scaffold through the generation of 12 previously unreported analogues and, together with previous results, permitted assignment of the ten methyltransferases required for everninomicin biosynthesis. The in vitro activity of A1- and H-ring-modifying methyltransferases demonstrated the ability to catalyze late-stage modification of the scaffold on an A1-ring phenol and H-ring C-4’ hydroxy moiety. Together these results establish the potential of the everninomicin scaffold for modification through mutagenesis and in vitro modification of advanced biosynthetic intermediates. 相似文献
4.
Poly(L-ornithine)s having various azo-contents in the side chains were synthesized by the water-soluble carbodiimide procedure. The photochemical properties of the polypeptides poly[Nδ-p-(phenylazo)benzoyl-L-ornithine] (PPABLO) containing 3–77 mol% azobenzene were investigated by absorption and circular dichroism spectroscopy in hexafluoro-2-propanol (HFIP) or water, and in HFIP-water or methanol-water solvent mixtures. The photochromism of the dichroic bands of the PPABLOs containing 20–77 mol% azobenzene in the visible and ultraviolet wavelength regions was found to be mostly reversible as a function of irradiation time at different wavelengths due to the photostationary state (above 80% trans-cis photoisomerization) of the azo aromatic moieties. The PPABLO containing 3.2 mol% azobenzene in water exhibited conformational changes from random coil to helix by the addition of methanol or sodium dodecyl sulphate (SDS). The photo-induced conformational change was observed in HFIP-water-SDS solvent mixtures, while no conformational change was seen in water and HFIP-water solvent mixtures. 相似文献
5.
Sandra L. McLellan Erika J. HollisMorgan M. Depas Meredith Van DykeJosh Harris Caitlin O. Scopel 《Journal of Great Lakes research》2007,33(3):566-580
Escherichia coli distribution and persistence in nearshore Lake Michigan were assessed following heavy rains and sanitary sewer overflow (SSO) and combined sewer overflow (CSO) events over a 5-year period, including an 18-day period following 25.4 cm of rainfall in which intensive studies were conducted following multiple CSO and SSO events. E. coli levels in the Milwaukee estuary and harbor following SSO and CSO events ranged from 104 to nearly 105 CFU/100 mL, which were significantly higher (p ≤ 0.05) than levels following rainfall alone. Sites outside of the breakwall but within the contamination plume (e.g., within 2 km of the harbor) were an order of magnitude lower. Locations 2–5 km from the harbor ranged from below detection limits, of < 1 to 5 CFU/100 mL. E. coli levels corrected for dilution based on specific conductivity measurements were lower than what would be expected for loss due to dilution alone, suggesting a combination of die-off and dilution, were responsible for the rapid disappearance of these organisms outside of the harbor. E. coli and fecal coliforms measured concurrently demonstrated that fecal coliforms could be recovered longer than E. coli in the open waters of the lake. E. coli isolated directly from sewage treatment plant influent were found to have a marked increase in antibiotic resistance traits for ten antibiotics commonly used in the human population compared with isolates from two animal sources of fecal pollution. However, E. coli obtained from sewage impacted water (n = 2,513) and from stormwater impacted water (n = 1,465) collected the previous year when there were no sewage overflows, were found to have no significant difference (p < 0.05) in the frequency of resistance when comparing the two conditions. E. coli survival characteristics and population dynamics are most likely influenced by multiple factors in complex systems such as the watershed/estuarine/lake environments of the Great Lakes. 相似文献
6.
Dora Szabo Zsolt Sarszegi Beata Polgar Eva Saghy Adam Nemeth Dora Reglodi Andras Makkos Aniko Gorbe Zsuzsanna Helyes Peter Ferdinandy Robert Herczeg Attila Gyenesei Attila Cziraki Andrea Tamas 《International journal of molecular sciences》2021,22(6)
Acute myocardial infarction (MI) is one of the most common causes of death worldwide. Pituitary adenylate cyclase activating polypeptide (PACAP) is a cardioprotective neuropeptide expressing its receptors in the cardiovascular system. The aim of our study was to examine tissue PACAP-38 in a translational porcine MI model and plasma PACAP-38 levels in patients with ST-segment elevation myocardial infarction (STEMI). Significantly lower PACAP-38 levels were detected in the non-ischemic region of the left ventricle (LV) in MI heart compared to the ischemic region of MI-LV and also to the Sham-operated LV in porcine MI model. In STEMI patients, plasma PACAP-38 level was significantly higher before percutaneous coronary intervention (PCI) compared to controls, and decreased after PCI. Significant negative correlation was found between plasma PACAP-38 and troponin levels. Furthermore, a significant effect was revealed between plasma PACAP-38, hypertension and HbA1c levels. This was the first study showing significant changes in cardiac tissue PACAP levels in a porcine MI model and plasma PACAP levels in STEMI patients. These results suggest that PACAP, due to its cardioprotective effects, may play a regulatory role in MI and could be a potential biomarker or drug target in MI. 相似文献
7.
Bernhard Kienesberger Beate Obermüller Georg Singer Barbara Mittl Reingard Grabherr Sigrid Mayrhofer Stefan Heinl Vanessa Stadlbauer Angela Horvath Wolfram Miekisch Patricia Fuchs Ingeborg Klymiuk Holger Till Christoph Castellani 《International journal of molecular sciences》2021,22(12)
We aimed to assess the in vitro antimicrobial activity and the in vivo effect on the murine fecal microbiome and volatile organic compound (VOC) profile of (S)-reutericyclin. The antimicrobial activity of (S)-reutericyclin was tested against Clostridium difficile, Listeria monocytogenes, Escherichia coli, Enterococcus faecium, Staphylococcus aureus, Staphylococcus (S.) epidermidis, Streptococcus agalactiae, Pseudomonas aeruginosa and Propionibacterium acnes. Reutericyclin or water were gavage fed to male BALBc mice for 7 weeks. Thereafter stool samples underwent 16S based microbiome analysis and VOC analysis by gas chromatography mass spectrometry (GC-MS). (S)-reutericyclin inhibited growth of S. epidermidis only. Oral (S)-reutericyclin treatment caused a trend towards reduced alpha diversity. Beta diversity was significantly influenced by reutericyclin. Linear discriminant analysis Effect Size (LEfSe) analysis showed an increase of Streptococcus and Muribaculum as well as a decrease of butyrate producing Ruminoclostridium, Roseburia and Eubacterium in the reutericyclin group. VOC analysis revealed significant increases of pentane and heptane and decreases of 2,3-butanedione and 2-heptanone in reutericyclin animals. The antimicrobial activity of (S)-reutericyclin differs from reports of (R)-reutericyclin with inhibitory effects on a multitude of Gram-positive bacteria reported in the literature. In vivo (S)-reutericyclin treatment led to a microbiome shift towards dysbiosis and distinct alterations of the fecal VOC profile. 相似文献
8.
9.
美洛西林钠的合成 总被引:1,自引:0,他引:1
陈凤英 《高校化学工程学报》2003,17(4):448-450
美洛西林钠是一种新型半合成青霉素。在以往的文献中其合成过程中都要使用剧毒品光气作为反应物。今以2-咪唑烷酮为起始原料,经甲磺酰化、酰化等四步反应,合成了酰脲类青霉素美洛西林钠。在合成过程中用氯甲酸三氯甲酯替代光气对其重要中间体l-氯甲酰基-3-甲磺酰基-2-咪唑烷酮的合成工艺进行了改进,不仅避免了使用光气,而且收率也从文献值70%提高到75%。 相似文献
10.