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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   
3.
This paper presents a simple alternative for an electronic ballast operating in self-sustained oscillating mode with dimming capability for fluorescent lamps. A simple modification in one of the gate drivers side circuit allows the lamp to dim without compromising the simplicity, reliability, and low cost which characterize the self-oscillating electronic ballast (SOEB). A qualitative analysis is presented to explain the behavior of the proposed self-oscillating electronic ballast with dimming feature. In addition, the stability and the key equations for the design are derived using the extended Nyquist criterion and describing function method. Experimental results from two 40-W electronic ballasts are presented to demonstrate the performance and to validate the analysis carried out.  相似文献   
4.
The internal anal sphincterotomy operation represents the best therapy for the treatment of those anal lesions, above all anal fissures, which cause hypertrophy and spasms of the internal anal sphincter. The Authors report their experience of 253 operations of internal subcutaneous sphincterotomy carried out between 1989 and 1995 under local anaesthesia in the outpatient clinic. The excellent results achieved prove that the procedure can easily be carried out under local anaesthesia in an outpatient clinic and, therefore, it is preferable to the surgical technique of isolation of the internal sphincter, not only for its practicality but also for the improved results.  相似文献   
5.
A novel directive and nondispersive antenna is presented: the ultrawideband (UWB) leaky lens. It is based on the broad band Cherenkov radiation occurring at a slot printed between different infinite homogeneous dielectrics. The first part of the paper presents the antenna concept and the UWB design. The issues that are specifically addressed include the impedance matching, the radiation pattern and the phase purity. Subsequently the hardware demonstrator and the results of the measurement campaign are shown. The results fully validate the antenna concept. The antenna presents decade bandwidth impedance matching, directive and frequency independent patterns in the H-plane over two octaves, negligible cross-polarization levels, weak amplitude dispersivity and, according to the authors, the most stable phase center for a directive antenna over an ultra wide frequency range.  相似文献   
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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   
8.
Absorption and distribution of polyunsaturated fatty acids was investigated in rats receiving lysophospholipids per os (30 mg kg-1). Lysophosphatidylcholine (lysoPC) increased [3H]arachidonate absorption and its incorporation into mucosal phosphatidylcholine. Transport of [3H]arachidonate by the phospholipid fraction of lymph lipoproteins and the level of [3H]arachidonate in plasma and liver lipids was also increased by lyso PC. Lysophosphatidylserine also increased [3H]arachidonate absorption but channeled the fatty acids into the aminophospholipid fraction of mucosal phospholipids, thus decreasing its efflux in lymph lipoproteins. As a consequence, lysophosphatidylserine caused [3H]arachidonate accumulation in mucosa. As similar results were obtained with [14C]linoleate, the data suggest that the addition of an appropriate lysophospholipid to the diet may direct absorption and distribution of polyunsaturated fatty acids.  相似文献   
9.
BACKGROUND: Nisin is a commercially available bacteriocin produced by Lactococcus lactis ATCC 11454 and used as a natural agent in the biopreservation of food. In the current investigation, milk whey, a byproduct from dairy industries was used as a fermentation substrate for the production of nisin. Lactococcus lactis ATCC 11454 was developed in a rotary shaker (30 °C/36 h/100 rpm) using two different media with milk whey (i) without filtration, pH 6.8, adjusted with NaOH 2 mol L?1 and without pH adjustment, both autoclaved at 121 °C for 30 min, and (ii) filtrated (1.20 µm and 0.22 µm membrane filter). These cultures were transferred five times using 5 mL aliquots of broth culture for every new volume of the respective media. RESULTS: The results showed that culture media composed of milk whey without filtration supplied L. lactis its adaptation needs better than filtrated milk whey. Nisin titers, in milk whey without filtration (pH adjusted), was 11120.13 mg L?1 in the second transfer, and up to 1628‐fold higher than the filtrated milk whey, 6.83 mg.L?1 obtained in the firstt transfer. CONCLUSIONS: Biological processing of milk byproducts (milk whey) can be considered a profitable alternative, generating high‐value bioproducts and contributing to decreasing river disposals by dairy industries. Copyright © 2008 Society of Chemical Industry  相似文献   
10.
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   
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