A series of 2-phenyloxazoles bearing an amide group at position 4 were designed and synthesized for evaluation as potential inhibitors of human recombinant monoamine oxidases (hrMAOs). Results of kinetics experiments demonstrated that all compounds behave as competitive MAO inhibitors, with good selectivity toward the MAO-B isoform. The most potent and selective derivatives are characterized by inhibition constant (Ki) values in the sub-micromolar range and a good selectivity index (Ki MAO-A/Ki MAO-B>50). Some derivatives were also found to be able to inhibit MAO activity in nerve growth factor (NGF)-differentiated PC12 cells, taken as a model of neuronal cells. In particular, 2-(2-hydroxyphenyl)-N-phenyloxazole-4-carboxamide (compound 4 a ) may be a promising new scaffold, exerting the highest selectivity and inhibitory effect toward MAOs in NGF-differentiated PC12 cell lysates, without compromising cell viability. Molecular docking analysis allowed a rationalization of the experimentally observed binding affinity and selectivity. 相似文献
Summary Circular dichroism of isotactic samples of poly-(S)-4-methyl-1-hexene and poly-(R)-3,7-dimethyl-1-octene, have been measured in the vacuum ultraviolet spectral region (200-140 nm). The c.d. band at about 160. nm accounts for the optical activity in the visible region and reflects the presence of one screw sense helical conformation of the sample examined.The authors thank Prof. W.C. Johnson, Jr., Department of Biochemistry and Biophysics, Oregon State University, for allowing them to use the vacuum u.v. spectrometer. This work has been partially supported by a N.A.T.O. grant, and by Ministero Pubblica Istruzione (MPI), Roma — Italy. 相似文献
CPP-TRS (Tonfoni 1989–94) is both a methodology and a language. Through the methodology (CPP — Communicative Positioning Program) those invisible aspects of communication are identified and represented by the meta-language (TRS — Text Representation Systems), which complements natural language. CPP-TRS is a new paradigm which applies to any communicative context.Icons in CPP-TRS are not intended to represent words or sentences in order to substitute them; they are rather intended to represent visually what natural language does not convey naturally. The improvement of communication is a challenge of the present and the future: CPP-TRS is designed explicitly for it.The CPP-TRS system thus is able to support the user with a set of visual tools, that are specifically suited to structuring text and communicating effectively.The same tools can support communication very effectively in situations where ambiguity can highly compromise the final result.The system may be used in a way that is either opaque or transparent to the reader of the text.Author of CPP-TRS¢ and CPP-TRS¢ Applications Designer. 相似文献
Calcium sulfoaluminate and Portland cement pastes, both prepared with a water/solid mass ratio equal to 0.5 and cured for time periods comprised between 2 h and 28 days, show completely different pore size distributions by mercury intrusion. Portland cement pastes aged at 12 h and 1 day exhibit a unimodal distribution of pore sizes related to a continuous network of capillary pores with a threshold pore radius decreasing from nearly 650 to 350 nm. After 7 and 28 days of curing, this parameter shifts to about 150 nm and a region having smaller pores appears (with a second threshold pore radius roughly comprised between 10 and 30 nm), made discontinuous by blockages of hydration products which occlude the interconnected pore system and isolate the interior space. For calcium sulfoaluminate cement pastes, a bimodal distribution is rapidly established, in which the regions with a lower porosity (threshold pore radii up to about 25 nm) are dominant, while the decrease of total porosity almost ceases at later ages. The porosimetric behaviour of calcium sulfoaluminate-based cement is related to its very fast hydration rate and to the lack of water needed to continue the hydration reactions. 相似文献
In an era characterized by fast technological progress that introduces new unpredictable scenarios every day, working in the law field may appear very difficult, if not supported by the right tools. In this respect, some systems based on Artificial Intelligence methods have been proposed in the literature, to support several tasks in the legal sector. Following this line of research, in this paper we propose a novel method, called PRILJ, that identifies paragraph regularities in legal case judgments, to support legal experts during the redaction of legal documents. Methodologically, PRILJ adopts a two-step approach that first groups documents into clusters, according to their semantic content, and then identifies regularities in the paragraphs for each cluster. Embedding-based methods are adopted to properly represent documents and paragraphs into a semantic numerical feature space, and an Approximated Nearest Neighbor Search method is adopted to efficiently retrieve the most similar paragraphs with respect to the paragraphs of a document under preparation. Our extensive experimental evaluation, performed on a real-world dataset provided by EUR-Lex, proves the effectiveness and the efficiency of the proposed method. In particular, its ability of modeling different topics of legal documents, as well as of capturing the semantics of the textual content, appear very beneficial for the considered task, and make PRILJ very robust to the possible presence of noise in the data.
A complete set up of optimal process conditions for an effective colloidal lithography/catalyst assisted MOCVD process integration is presented. It mainly focuses on the determination of the deposition temperature threshold for ZnO Metal-Organic Chemical Vapour Deposition (MOCVD) as well as the concentration of metal-organic silver (Ag) catalyst. Indeed, the optimization of such process parameters allows to tailor the ZnO film morphology in order to make the colloidal lithography/catalyst assisted MOCVD approach a valuable bottom up method to fabricate bi-dimensional ordered ZnO nanohole arrays. 相似文献
Sugar content is one of the most important quality attributes of citrus fruit, either for fresh or for processing market.
Since sugars in citrus juice are highly correlated with total soluble solids (TSS) content, which can be determined easily
even by the means of a hand refractometer, TSS is one of the most frequently used quality index. Since TSS can be measured
only destructively, the results are representative only if carried out on large samples and do not allow classifying marketable
fruit one by one according to their specific sugar content. Objective of this experiment was to assess possibility and limits
of a non-destructive estimation of citrus fruits internal quality parameters (TSS and titratable acidity) presenting thick
peel by the use of a spectrophotometric portable VIS-NIR system. Four hundred fruit of “Miho” satsuma and 150 fruit of “Page”
tangelo were used. Each fruit was first subjected to spectrophotometric acquisition and soon after was juiced and TSS and
titratable acidity (TA) determined. Partial least squares (PLS) regression analysis was applied for constructing a predictive
model based on the spectral normalized response, constructing the model on a sub-sample and verifying the model (prediction
test) on independent ones. The TA relative to Page mandarin was predicted in the test with an r = 0.88 and a standard error of prevision (SEP) coefficient of variability of 3.8% while the TSS scored an r = 0.85 and a SEP coefficient of variability equal to 4%. The TA of Miho mandarin was predicted in the test with an r = 0.81 and a SEP coefficient of Variability of 8.3% while the TSS scored an r = 0.84 and a SEP coefficient of variability equal to 5.6%. 相似文献
Fruit maturity indexes are crucial in harvest time determination and commercial context. The harvest time of apples, matching
the desired commercial characteristics, is assessed through starch–iodine test in practice. Fruit halves are dipped into iodine
solution and patterns are visually evaluated by experts comparing them to reference charts. Aim of the work was to study the
relationships of near infrared (NIR) spectral images (1,000–1,700 nm), starch/starch-free patterns visually assessed and RGB
color images. Spectral images of 88 Golden Delicious Klon B apples were sampled at seven different maturity stages. Partial
least-squares discriminant analysis (PLSDA) technique was used on hyper-spectral NIR images to classify single pixels using
its NIR reflectance spectrum. The response variable (i.e. the classification for each pixel) was identified through the matching
of single pixel obtained with the color images, segmented in two classes (starch and starch-free), and the NIR hyper-spectral
matrix. Mean hyper-spectral classification obtained through PLSDA modeling on individual apple correctly classified 80.81%
of the total pixels, while the unique model, i.e. a single model including all the fruits, resulted in 66.33%. In the latter
case, the relationship with the RGB classification showed high values (Pearson correlation coefficient r = 0.95). The present work shows the feasibility of NIR imaging spectroscopy as a tool for apple fruit maturity determination,
avoiding expert’s subjective interpretation by traditional starch index assignments. 相似文献
The objective of this study was to evaluate the effects of starch source and amylose content on the expansion ratio, density, and texture of expanded extrudates, as well as to investigate the structural and molecular changes that occur in starch granules as a function of extrusion. The starches employed were rice starches (8%, 20%, and 32% amylose), carioca bean starch (35% amylose), and Hylon V® corn starch (55% amylose). The extrudates from rice starches containing 20% and 32% amylose exhibited the highest expansion ratio, while, extrudates from Hylon V® corn starch containing 55% amylose exhibited the lowest expansion ratio. The hardness values of the extrudates with 55% amylose were twice those of the extrudates with 20%, 32%, and 35% amylose. An additional finding was that although the amylopectin promoted the expansion of the gelatinized starch matrix, it failed to strengthen and sustain the walls of the extrudate bubbles during expansion. 相似文献