Chemotherapeutic agents. XII [1]. Synthesis of Pyrimidines and Fused Pyrimidines as leishmanicides and herbicides

Various bicyclic ( 2 , 3 ) and tricyclic ( 4 , 5 ) heterocycles were prepared by the reaction of 1a , c with dihaloalkanes and polynitrohalobenzene separately. Electrophilic substitution on 1a–c with different alkyl halides yielded mono and dialkyl pyrimidiens ( 6–20 ). Nucleophilic substitution reactions on 18 and 21 with amine and hydrazine separately yielded 22–31 , 21a , b and 41c . Reaction of 25a with ethyl ethoxymethylenecyanoacetate and chloroacetyl chloride separately provided bicyclic compounds 32 and 33 . Condensation-cyclization of 25a with formic, acetic and nitrous acid separately yielded 34a , b and 35 . Reaction of 26a with ethylthiocylycolate and thiourea separately provided 36a and 39 . The latter was alkylated with methyl iodide to 40 . An attempt to cyclize 29a and 30a with thionyl chloride provided bicyclic compounds 37a , b and an uncyclic product 38 . Some of the compounds were screened for leishmanicidal and herbicidal activities and a few of them exhibited significant activity. Leishmaniasis is considered to be one of the most devastating diseases and is ominous to tropical countries. The high toxicity of leishmanicidal drugs in current use, aroused considerable interest to develop new safer and effective chemotherapeutic agents. The only drug pyrimethamine [2] is the representative of pyrimidine derivatives, known as leishmanicides but low order of activity at high dose failed to retain in the clinic. Based on our past experiences in rational designing of leishmanicidal pyrimidine analogs, incorporation of levamisole pharmacophore either in flexible or rigid forms is indispensable for potential activity [1,3] against visceral leishmaniasis. These observations induced an impetus to synthesize pyrimidine analogs as potential leishmanicides.     

The effect of microencapsulated phase change materials on the rheology of geopolymer and Portland cement mortars

The effect of microencapsulated phase-change materials (MPCM) on the rheological properties of pre-set geopolymer and Portland cement mortars was examined. Microcapsules with hydrophilic and hydrophobic shells were compared. The shear rate dependency of the viscosities fitted well to a double Carreau model. The zero shear viscosities are higher for geopolymer mortar, illustrating poorer workability. The time evolution of the viscosities was explored at shear rates of 1 and 10 s⁻¹. New empirical equations were developed to quantify the time-dependent viscosity changes. The highest shear rate disrupted the buildup of the mortar structures much more than the lower shear rate. Microcapsules with a hydrophobic shell affect the rheological properties much less than the microcapsules with a hydrophilic shell, due to the higher water adsorption onto the hydrophilic microcapsules. Shear forces was found to break down the initial structures within geopolymer mortars more easily than for Portland cement mortars, while the geopolymer reaction products are able to withstand shear forces better than Portland cement hydration products. Initially, the viscosity of geopolymer mortars increases relatively slowly during due to formation of geopolymer precursors; at longer times, there is a steeper viscosity rise caused by the development of a 3D-geopolymer network. Disruption of agglomerates causes the viscosities of portland cement mortars to decrease during the first few minutes, after which the hydration process (increasing viscosities) competes with shear-induced disruption of the structures (decreasing viscosities), resulting in a complex viscosity behavior.     

Consolidation of advanced composites having volatile generation

Processing polyimide-based thermosetting matrix composites is complicated because of gaseous volatiles produced during the polymerization and crosslinking reactions. This process involves complex interactions between part geometry, temperature and force cycles, and matrix/fiber properties. A simple model for the consolidation process that treats these composites as a three-phase system consisting of fiber, resin, and volatile has been developed. This model has been applied to compression molding process for constant thickness laminates and the predictions agree well with experiments. Further extension to handle three-dimensional parts and the required numerical techniques have also been developed.     

Melt processing of ethylene–vinyl acetate/banana starch/Cloisite 20A organoclay nanocomposite films: structural,thermal and composting behavior

This work shows the preparation of ethylene vinyl acetate copolymer/banana starch/Cloisite 20A organoclay (EVA/starch/C20A) nanocomposites by melt processing. Wide angle X-ray diffraction (WAXD), field emission scanning electron microscopy (FE-SEM), differential scanning calorimetry and thermogravimetric analysis were used to characterize the obtained nanocomposites. Mechanical properties were also determined. In addition, the performance of the nanocomposite films under composting was preliminarily studied; it was conducted using the soil burial test method. Despite knowing that the starch is difficult to process by extrusion, nanocomposite films with high homogeneity were obtained. In this case, C20A organoclay acts as an effective surfactant to make the starch natural polymer compatible with the EVA synthetic polymer. The good compatibility between EVA, starch and C20A clay was also deduced by the formation of intercalated and intercalated-exfoliated structures determined by WAXD and FE-SEM. Physical evidence of the damage in EVA/starch/C20A nanocomposite films after the composting test was observed. It is worth noting that despite the absence of starch, the EVA/C20A nanocomposite film, used as a control, also showed surface damage. This behavior is related to the organic modifier linked to clay C20A, which contains molecules derived from fatty acids that can be used as a food source for microorganisms.

     

Design of vessels subjected to external pressure

An analytical procedure, developed to simulate the graphic method for the design of vessels subjected to external pressure or vacuum, suggested by the ASME Code, Section VIII, Division 1, is presented in this contribution. A comprehensive computer program based on this method is also presented. The program also covers the design of stiffener rings. The procedure can be easily extended to include other international standards such as the British and German codes, since the method is based on the concept of the number of lobes at collapse. The method produced reproducible results over the entire range of L/D₀ and D₀/t ratios of the code. The deviation observed at any point in this range is less than 0.5% for factor A. The variation in allowable pressure is less than 2%.     

Mining the Wheat Grain Proteome

Bread wheat is the most widely cultivated crop worldwide, used in the production of food products and a feed source for animals. Selection tools that can be applied early in the breeding cycle are needed to accelerate genetic gain for increased wheat production while maintaining or improving grain quality if demand from human population growth is to be fulfilled. Proteomics screening assays of wheat flour can assist breeders to select the best performing breeding lines and discard the worst lines. In this study, we optimised a robust LC–MS shotgun quantitative proteomics method to screen thousands of wheat genotypes. Using 6 cultivars and 4 replicates, we tested 3 resuspension ratios (50, 25, and 17 µL/mg), 2 extraction buffers (with urea or guanidine-hydrochloride), 3 sets of proteases (chymotrypsin, Glu-C, and trypsin/Lys-C), and multiple LC settings. Protein identifications by LC–MS/MS were used to select the best parameters. A total 8738 wheat proteins were identified. The best method was validated on an independent set of 96 cultivars and peptides quantities were normalised using sample weights, an internal standard, and quality controls. Data mining tools found particularly useful to explore the flour proteome are presented (UniProt Retrieve/ID mapping tool, KEGG, AgriGO, REVIGO, and Pathway Tools).     

Introducing the Planar Laser-Induced Fluorescence Technique (PLIF) to Measure Mixing Time in Gas-Stirred Ladles

Metallurgical and Materials Transactions B - The planar laser-induced fluorescence (PLIF) technique was implemented to measure mixing time in a 1/17 water model of a 200-ton ladle furnace. The...     

流态化冷却器创新改进设计及应用

针对流态化冷却器在运行中出现的水套易开裂、观察孔盖无法正常打开、窥视孔盖密封失效、进料插板阀无法正常切换及开闭等问题,云南驰宏锌锗股份有限公司提出相应的改进措施.改造后,水套焊缝寿命延长到12个月,窥视孔盖密封使用12个月后仍未失效,进料插板阀密封无泄漏,从而提高了设备使用寿命,保障了设备稳定运行.     

Antimicrobial resistance and phage and molecular typing of Salmonella strains isolated from food for human consumption in Spain

The aims of this study were to ascertain the population structure and antimicrobial susceptibility of Salmonella enterica serovars isolated in 2002 from food in 16 Spanish regions. Serovars were characterized by serotyping, phage typing, antimicrobial susceptibility, and pulsed-field gel electrophoresis (PFGE) typing, and 264 nonrelated strains were selected for further analysis. The main sources were eggs and their derivatives (21.6% of strains), poultry and related products (16.6%), and seafood (16.3%). High serotype diversity was detected (51 serotypes); the most common were Enteritidis (n = 96, 36.3%) and Typhimurium (n = 53, 20.1%), followed by a miscellaneous group of 49 different serotypes (n = 115, 43.5%). A 15% increase in Salmonella Enteritidis isolation was observed. Common phage types for Salmonella Enteritidis were PT1 (41.6% of isolates), PT4 (9.4%), PT6 (9.4%), and PT6a (9.4%), and common types for Salmonella Typhimurium were DTU302 (18.8%), DT104 (15.1%), and DT104B (13.2%). Salmonella Enteritidis strains were categorized into eight PFGE types with a similarity of 81 to 96%, and 73.9% of the strains were grouped into just one cluster. Salmonella Typhimurium isolates were divided into 13 PFGE types with a similarity of 64 to 86%, and one predominant clone contained 41.5% of the strains. Resistance rates for Salmonella Enteritidis, Salmonella Typhimurium, and the miscellaneous group were, respectively, 8.3, 69.8, and 13.9% for ampicillin, 3.1, 52.8, and 59% for streptomycin, 40.6, 22.6, and 10.4% for nalidixic acid, 15.6, 71.7, and 31.1% for tetracycline, 7.3, 18.8, and 9.5% for trimethoprim-sulfamethoxazole, 0, 50.9, and 4.3% for chloramphenicol, and 6.2, 71.7, and 17.4% for multiple (at least four) antimicrobials. All the strains remained susceptible to other beta-lactams and fluoroquinolones. Surveillance of S. enterica isolated from food is strongly recommended to reduce community exposure to antimicrobial resistant strains.     

Isolation and characterization of Shiga toxin-producing Escherichia coli O157:H7 and non-O157 from beef carcasses at a slaughter plant in Mexico

The contamination of beef carcasses with Shiga toxin-producing O157:H7 and non-O157 Escherichia coli (STEC) obtained from a slaughter plant in Guadalajara, Mexico was investigated. A total of 258 beef carcasses were sampled during a 12-month period. All samples were assayed for STEC by selective enrichment in modified tryptone soy broth supplemented with cefixime, cefsulodin and vancomycin, followed by plating on Sorbitol MacConkey Agar supplemented with cefixime and tellurite (CT-SMAC). Simultaneously, all samples were assayed by immunomagnetic separation (IMS) and plated on CT-SMAC and CHROMagar. The presence of the stx1, stx2, eaeA and hly933 genes, recognized as major virulence factors of STEC, was tested for O157:H7 and non-O157 E. coli isolates by multiplex polymerase chain reaction (PCR). STEC was detected in two (0.8%) samples. One of these STEC isolates corresponded to the serotype O157:H7 showing stx2, eaeA and hyl933 genes. The other isolate corresponded to non-O157 STEC and only had the stx1 gene. Thirteen carcasses (5%) were positive for nonmotile E. coli O157 and 7 (2.7%) were positive for E. coli O157:H7. The presence of O157:H7 and non-O157 STEC on beef carcasses in this slaughter plant in Guadalajara, Mexico, emphasizes the importance of implementing the Hazard Analysis and Critical Control Point (HACCP) system, as well as the need for implementing, evaluating, and validating antimicrobial interventions to reduce the presence of potential pathogenic microorganisms.