可溶性汞化苯乙烯－丙烯酸甲酯共聚物的合成

用自由基溶液降合方法制备一系列苯乙烯－丙烯酸甲酯线型共聚物，用核磁共振测定了苯基在共聚物中的百分比，在该共聚物的四氢呋喃溶液中，用三氟乙酸汞在共聚物的苯环上进行亲电取代反应，得到可溶性汞化共聚物，由于这类泵化共的可溶于四氢呋喃，二氯甲烷等溶剂，用重沉淀法多次提纯，得到了纯度很高，溶解性较好的含重金属二价汞的共聚物，用红外光谱仪测定共聚物上的汞基团，用原子吸收定量测试共聚中的汞的百分聚代率，结果表明     

Using chemical probes to investigate the sub-inhibitory effects of azithromycin

The antibacterial drug azithromycin has clinically beneficial effects at sub-inhibitory concentrations for the treatment of conditions characterized by chronic Pseudomonas aeruginosa infection, such as cystic fibrosis. These effects are, in part, the result of inhibition of bacterial biofilm formation. Herein, the efficient synthesis of azithromycin in 4 steps from erythromycin and validation of the drug's ability to inhibit biofilm formation at sub-MIC (minimum inhibitory concentration) values are reported. Furthermore, the synthesis of immobilized and biotin-tagged azithromycin analogues is described. These chemical probes were used in pull-down assays in an effort to identify azithromycin's binding partners in vivo. Results from these assays revealed, as expected, mainly ribosomal-related protein binding partners, suggesting that this is the primary target of the drug. This was further confirmed by studies using a P. aeruginosa strain containing plasmid-encoded ermC, which expresses a protein that modifies 23S rRNA and so blocks macrolide entry to the ribosome. In this strain, no biofilm inhibition was observed. This work supports the hypothesis that the sub-inhibitory effects of azithromycin are mediated through the ribosome. Moreover, the synthesis of these chemical probes, and proof of their utility, is of value in global target identification in P. aeruginosa and other species.     

Synthesis and stability of small molecule probes for Pseudomonas aeruginosa quorum sensing modulation

The human pathogen Pseudomonas aeruginosa uses N-butyryl-L-homoserine lactone (BHL) and N-(3-oxododecanyl)-L-homoserine lactone (OdDHL) as small molecule intercellular signals in a phenomenon known as quorum sensing (QS). QS modulators are effective at attenuating P. aeruginosa virulence; therefore, they are a potential new class of antibacterial agent. The lactone in BHL and OdDHL is hydrolysed under physiological conditions. The hydrolysis proceeds at a rate faster than racemisation of the alpha-chiral centre. Non-hydrolysable, non-racemic analogues (small molecule probes) were designed and synthesised, replacing the lactone with a ketone. OdDHL analogues were found to be relatively unstable to decomposition unless they were difluorinated between the beta-keto amide. Stability studies on a non-hydrolysable, cyclohexanone analogue indicated that racemisation of the alpha-chiral centre was relatively slow. This analogue was assayed to show that the L-isomer is likely to be responsible for the QS autoinducing activity in P. aeruginosa and Serratia strain ATCC39006.     

Axisymmetric trawl cod-ends made from netting of a generalized mesh shape

The equations governing the geometry of axisymmetric trawl cod-endsmade from netting of meshes of a particular generalized structureare derived. From this, by suitable setting of the initial meshbar lengths, the equations governing the geometry of cod-endsthat are of importance to the fishing industry can be readilydeduced. It is assumed that arbitrary membrane forces act normalto the edges of the mesh elements, that there is no shear forceacting on the edge of a mesh element and that the twine thatmakes up the netting is extensible. The case where there isslackness in the mesh bars in the circumferential directionis dealt with and it is demonstrated how the finite structureof a knot can be taken into account. The case where the membraneforces arise solely as a result of and can be expressed by theappropriate components of the tensions in the mesh bars is alsoexamined and numerical solutions are found for a range of examples.