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1.
The paper presents a survey of the contamination level of the Danube river sediments along its course, between 849 km and 1162 km, during the period 1985–1988. Sampling was performed on several locations in the seasons with extreme hydrological conditions (spring, autumn). 相似文献
2.
Construction of a New Class of Tetracycline Lead Structures with Potent Antibacterial Activity through Biosynthetic Engineering
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Dr. Urška Lešnik Dr. Tadeja Lukežič Dr. Ajda Podgoršek Dr. Jaka Horvat Dr. Tomaž Polak Dr. Martin Šala Branko Jenko Dr. Kirsten Harmrolfs Dr. Alain Ocampo‐Sosa Prof. Dr. Luis Martínez‐Martínez Dr. Paul R. Herron Dr. Štefan Fujs Dr. Gregor Kosec Prof. Dr. Iain S. Hunter Prof. Dr. Rolf Müller Prof. Dr. Hrvoje Petković 《Angewandte Chemie (International ed. in English)》2015,54(13):3937-3940
Antimicrobial resistance and the shortage of novel antibiotics have led to an urgent need for new antibacterial drug leads. Several existing natural product scaffolds (including chelocardins) have not been developed because their suboptimal pharmacological properties could not be addressed at the time. It is demonstrated here that reviving such compounds through the application of biosynthetic engineering can deliver novel drug candidates. Through a rational approach, the carboxamido moiety of tetracyclines (an important structural feature for their bioactivity) was introduced into the chelocardins, which are atypical tetracyclines with an unknown mode of action. A broad‐spectrum antibiotic lead was generated with significantly improved activity, including against all Gram‐negative pathogens of the ESKAPE panel. Since the lead structure is also amenable to further chemical modification, it is a platform for further development through medicinal chemistry and genetic engineering. 相似文献
3.
Salas G Podgoršek A Campbell PS Santini CC Pádua AA Costa Gomes MF Philippot K Chaudret B Turmine M 《Physical chemistry chemical physics : PCCP》2011,13(30):13527-13536
Ionic liquids are a stabilizing medium for the in situ synthesis of ruthenium nanoparticles. Herein we show that the addition of molecular polar solutes to the ionic liquid, even in low concentrations, eliminates the role of the ionic liquid 3D structure in controlling the size of ruthenium nanoparticles, and can induce their aggregation. We have performed the synthesis of ruthenium nanoparticles by decomposition of [Ru(COD)(COT)] in 1-butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide, [C(1)C(4)Im][NTf(2)], under H(2) in the presence of varying amounts of water or 1-octylamine. For water added during the synthesis of metallic nanoparticles, a decrease of the solubility in the ionic liquid was observed, showed by nanoparticles located at the interface between aqueous and ionic phases. When 1-octylamine is present during the synthesis, stable nanoparticles of a constant size are obtained. When 1-octylamine is added after the synthesis, aggregation of the ruthenium nanoparticles is observed. In order to explain these phenomena, we have explored the molecular interactions between the different species using (13)C-NMR and DOSY (Diffusional Order Spectroscopy) experiments, mixing calorimetry, surface tension measurements and molecular simulations. We conclude that the behaviour of the ruthenium nanoparticles in [C(1)C(4)Im][NTf(2)] in the presence of 1-octylamine depends on the interaction between the ligand and the nanoparticles in terms of the energetics but also of the structural arrangement of the amine at the nanoparticle's surface. 相似文献
4.
An alternative approach to the study of Jordan ideals in associative algebras is considered. The same method can be used when analogous questions in graded algebras are treated. 相似文献
5.
Quantitative data for some of the radionuclides, most important because of their intensity and radiotoxicity, present in the biosphere after the Chernobyl accident are given for a selected number among numerous plant and food samples analyzed before and after the accident. 相似文献
6.
The trend of variation of sediment radiocontamination, expressed as a function of space and time, and specific accumulation of particular radionuclides in some investigated localities, are discussed on the basis of experimental results of gamma spectrometric analyses of artificial radionuclide contents. 相似文献
7.
Serum paraoxonase-1 (PON1) is the most studied member of the group of paraoxonases (PONs). This enzyme possesses three enzymatic activities: lactonase, arylesterase, and paraoxonase activity. PON1 and its isoforms play an important role in drug metabolism as well as in the prevention of cardiovascular and neurodegenerative diseases. Although all three members of the PON family have the same origin and very similar amino acid sequences, they have different functions and are found in different locations. PONs exhibit substrate promiscuity, and their true physiological substrates are still not known. However, possible substrates include homocysteine thiolactone, an analogue of natural quorum-sensing molecules, and the recently discovered derivatives of arachidonic acid—bioactive δ-lactones. Directed evolution, site-directed mutagenesis, and kinetic studies provide comprehensive insights into the active site and catalytic mechanism of PON1. However, there is still a whole world of mystery waiting to be discovered, which would elucidate the substrate promiscuity of a group of enzymes that are so similar in their evolution and sequence yet so distinct in their function. 相似文献
8.
Empirical expression for experimentally obtained functional dependence between the results of total -activity and integral -activity activity of fallout, measured during May, 1986, at a control point: 44°47 northern latitude and 20°32 eastern longitude, has been established in order to enable estimation of the level of fallout contamination by -emitters when total -activity values are known. 相似文献
9.
The results of analysis of 15 samples of meat, eggs, feed and water used in the cycle of intensive poultry breeding are given
in the paper. Twenty chemical elements such as: Sm, Lu, Eu, Hf, Ce, Yb, Cr, La, Br, Sb, Cs, Sc, Fe, Co, Na, Ta, Tb, Zr, Rb
and Zn have been quantitatively determined in all the samples by nondestructive neutron activation analysis. Qualitative determination
of K, Ca, Ru and Au was also performed in some samples. 相似文献
10.
Aequationes mathematicae - In this note we prove that every Jordan derivation on a triangular ring is a derivation. Moreover, we show that, under some conditions, every Jordan derivation on a... 相似文献