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21.
Dr. Eric M. Lewandowski Dr. Łukasz Szczupak Dr. Aleksandra Kowalczyk Dr. Gracia Mendoza Prof. Manuel Arruebo Lian M. C. Jacobs Prof. Paweł Stączek Prof. Yu Chen Prof. Konrad Kowalski 《Chembiochem : a European journal of chemical biology》2020,21(15):2187-2195
The conjugation of organometallic groups to current β-lactam antibiotics is a field of increasing study due to the ability of certain organometallic groups to enhance the antibiotic potency of these drugs. Herein, we report the antibacterial properties of two metallocenyl (ferrocenyl and ruthenocenyl) 7-aminocephalosporanic acid (7-ACA) antibiotic conjugates. Continuing a trend we found in our previous studies, the ruthenocenyl conjugate showed greater antibacterial activity than its ferrocenyl counterpart. Compared with the previously published 7-aminodesacetoxycephalosporanic acid (7-ADCA) conjugates, the 3-acetyloxymethyl group significantly improved the compounds’ activity. Furthermore, the Rc-7-ACA compound was more active against clinical Staphylococcus aureus isolates than the ampicillin reference. Noticeably, neither of the two new compounds showed an undesirable toxic effect in HeLa and L929 cells at the concentrations at which they displayed strong antibacterial effects. The antibacterial activity of the two metallocenyl 7-ACA derivatives was further confirmed by scanning electron microscopy (SEM). SEM micrographs showed that bacteria treated with metallocenyl 7-ACA derivatives feature cell wall damage and morphology changes. Using a CTX-M-14 β-lactamase competition assay based on nitrocefin hydrolysis, we showed that the Rc-7-ACA bound more favorably to CTX-M-14 than its ferrocenyl counterpart, again confirming the superiority of the ruthenocenyl moiety over the ferrocenyl one in interacting with proteins. We also report a 1.47 Å resolution crystal structure of Rc-7-ACA in complex with the CTX-M-14 E166A mutant, an enzyme sharing a similar active site configuration with penicillin-binding proteins, the molecular target of β-lactam antibiotics. These results strengthen the case for the antibacterial utility of the Rc and Fc groups. 相似文献
22.
Medel Manuel L. Zulueta Donala Janreddy Shang-Cheng Hung 《Israel journal of chemistry》2015,55(3-4):347-359
In recent years, there has been rapid expansion of glycan synthesis, fueled by the recognition that the structural complexity of sugars translates to a myriad of biological functions. Such chemical syntheses involve many challenges, mostly due to the regio- and stereochemical aspects of glycosidic bond formation. One-pot strategies were developed to assist in attaining faster and more economical access to the glycan constructs. In this front, achievements in protecting group manipulation, glycosylation, and combinations of these have been reported. Protecting group manipulations in one pot take advantage of the reaction compatibility of commonly used transformations, many of which occur in high regioselectivity. Sequential glycosylations, on the other hand, rely on leaving group orthogonalities and reactivity tuning, as well as the preactivation technique. Altogether, these approaches offer attractive means to the much needed glycan structures and, consequently, help usher in advances in glycoscience. 相似文献
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Mac Arturo Murillo Francisco J. Rodríguez‐Pulido Francisco J. Heredia Manuel Melgosa Jorge Pacheco Ronny Vargas Ernesto Montero Dionisio Gutirrez 《Color research and application》2019,44(2):160-167
Placebo white tablet cores (lactose anhydrous [47.6%], corn starch [23.8%], microcrystalline cellulose [19.1%], polyvinylpyrrolidone [7.9%], magnesium stearate [0.8%], and talcum powder [0.8%]) were coated with a colorant (hydroxypropyl methylcellulose [8% w/v], titanium dioxide [0.2% w/v], FD&C yellow No. 6 with aluminum lacquer [0.8% w/v], polyethylene glycol 4000 [0.4% w/v], and purified water [q.s.p. 100 mL]) using a random spraying method during 130 minutes. During the coating process, batches of 21 samples were extracted every 10 minutes and measured with a DigiEye imaging system. The initial cores showed very similar and uniform colors (Mean Color Difference from the Mean [MCDM] of 0.8 CIELAB units), but partially coated tablets showed lower uniformity (MCDM below 2.0 CIELAB units). There was a high color variability (MCDM about 4.0 CIELAB units) among tablets of the same batch in the period between 10 and 30 minutes, which decreased as the coating process progressed, until achieving a final acceptable value (MCDM below 2.0 CIELAB units). During the coating process, L* decreased, C*ab strongly increased, and h ab remained nearly constant (disregarding results at 0 and 10 minutes). CIELAB and CIEDE2000 color differences (mainly chroma differences) with respect to the initial color of the tablets were modeled as a function of time by exponential functions with three coefficients. The color change in the interval from 90 to 130 minutes (4.3 CIELAB units, or 2.6 CIEDE2000 units), may be considered negligible bearing in mind the color variability in the batches of 21 samples and typical values of visual color thresholds. 相似文献
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Olías Manuel Cánovas Carlos R. Basallote M. Dolores 《Mine Water and the Environment》2021,40(1):235-249
Mine Water and the Environment - The failure of the tailing dam at the Aznalcóllar mine (SW Spain) in 1998 released ≈ 6 million m3 of pyrite sludge and acidic... 相似文献
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Castelo Gmez Juan Manuel Carrillo Mondjar Javier Roldn Gmez Jos Martnez Martnez Jos Luis 《International Journal of Information Security》2021,20(5):647-673
International Journal of Information Security - The weakness of the security measures implemented on Internet of Things (IoT) devices, added to the sensitivity of the data that they handle, has... 相似文献
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Binbin Chen Nicolas Gauquelin Daen Jannis Daniel M. Cunha Ufuk Halisdemir Cinthia Piamonteze Jin Hong Lee Jamal Belhadi Felix Eltes Stefan Abel Zoran Jovanović Matjaž Spreitzer Jean Fompeyrine Johan Verbeeck Manuel Bibes Mark Huijben Guus Rijnders Gertjan Koster 《Advanced materials (Deerfield Beach, Fla.)》2020,32(50):2004995
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Goyanes Manuel Demeter Márton Grané Aurea Albarrán-Lozano Irene Gil de Zúñiga Homero 《Scientometrics》2020,125(3):2299-2322
Scientometrics - With today’s research production and global dissemination, there is growing pressure to assess how academic fields foster diversity. Based on a mathematical problem/solve... 相似文献