In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compounds.

IMPORTANCE: The in vitro assessment of diruthenium(II)-arene compounds against Escherichia coli, Streptococcus pneumoniae, and Staphylococcus aureus showed a significant antibacterial activity of some compounds against S. pneumoniae, with minimum inhibitory concentration (MIC) values ranging from 1.3 to 2.6 µM, and a medium activity against E. coli, with MIC of 25 µM. The nature of the substituents anchored on the bridging thiols and the compounds molecular weight appear to significantly influence the antibacterial activity. Fluorescence microscopy showed that these ruthenium compounds enter the bacteria and do not accumulate in the cell wall of gram-positive bacteria. These diruthenium(II)-arene compounds exhibit promising activity against S. aureus and S. pneumoniae and deserve to be considered for further studies, especially the compounds bearing larger benzo-fused lactam substituents.

The DEPTQ+ Experiment: Leveling the DEPT Signal Intensities and Clean Spectral Editing for Determining CHn Multiplicities.

We propose a new 13C DEPTQ+ NMR experiment, based on the improved DEPTQ experiment, which is designed to unequivocally identify all carbon multiplicities (Cq, CH, CH2, and CH3) in two experiments. Compared to this improved DEPTQ experiment, the DEPTQ+ is shorter and the different evolution delays are designed as spin echoes, which can be tuned to different 1JCH values; this is especially valuable when a large range of 1JCH coupling constants is to be expected. These modifications allow (i) a mutual leveling of the DEPT signal intensities, (ii) a reduction in J cross-talk in the Cq/CH spectrum, and (iii) more consistent and cleaner CH2/CH3 edited spectra. The new DEPTQ+ is expected to be attractive for fast 13C analysis of small-to medium sized molecules, especially in high-throughput laboratories. With concentrated samples and/or by exploiting the high sensitivity of cryogenically cooled 13C NMR probeheads, the efficacy of such investigations may be improved, as it is possible to unequivocally identify all carbon multiplicities, with only one scan, for each of the two independent DEPTQ+ experiments and without loss of quality.

Ethylene application at the immature stage of Fragaria chiloensis fruit represses the anthocyanin biosynthesis with a concomitant accumulation of lignin.

Ethylene seems to play a secondary role in non-climacteric strawberry ripening compared to abscisic acid. However, this does not exclude that ethylene can regulate some specific events related to the ripening process. Preliminary experiments of applications of ethylene or its inhibitor 1-MCP to strawberry fruits have reinforced this hypothesis. Here, we reveal some previously non-covered physiological effects of ethylene using an in vitro strawberry ripening system. Fruits of Fragaria chiloensis treated with ethephon at the large green developmental stage showed inhibition of anthocyanin biosynthesis and downregulation of essential anthocyanin biosynthesis genes during the ripening. At the same time, ethylene stimulated lignin biosynthesis and remarkably upregulated the expression of FcPOD27. Since contrasting results have been reported when ethylene was applied at late ripening developmental stages, our findings support the hypothesis of a temporal-specific ethylene role in the ripening of strawberry fruits.

Radical chain monoalkylation of pyridines.

The monoalkylation of N-methoxypyridinium salts with alkyl radicals generated from alkenes (via hydroboration with catecholborane), alkyl iodides (via iodine atom transfer) and xanthates is reported. The reaction proceeds under neutral conditions since no acid is needed to activate the heterocycle and no external oxidant is required. A rate constant for the addition of a primary radical to N-methoxylepidinium >107 M-1 s-1 was experimentally determined. This rate constant is more than one order of magnitude larger than the one measured for the addition of primary alkyl radicals to protonated lepidine demonstrating the remarkable reactivity of methoxypyridinium salts towards radicals. The reaction has been used for the preparation of unique pyridinylated terpenoids and was extended to a three-component carbopyridinylation of electron-rich alkenes including enol esters, enol ethers and enamides.