5 research outputs found

    The 1991 3rd NASA Symposium on VLSI Design

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    Papers from the symposium are presented from the following sessions: (1) featured presentations 1; (2) very large scale integration (VLSI) circuit design; (3) VLSI architecture 1; (4) featured presentations 2; (5) neural networks; (6) VLSI architectures 2; (7) featured presentations 3; (8) verification 1; (9) analog design; (10) verification 2; (11) design innovations 1; (12) asynchronous design; and (13) design innovations 2

    Evaluation of the ingestive behaviour of the dairy cow under two systems of rotation with slope

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    The ingestive behaviour of grazing animals is modulated by the vegetation characteristics, topography and the type of stocking method. This research was carried out in 2019, at the Rumipamba CADER-UCE. It aimed to evaluate the impact of two contrasting stocking methods of dairy cows grazing a pasture with an average of slope >8.5%. Four dairy cows were set to graze a 0.4 ha paddock for 5 days for continuous stocking methods, while for the electric fence methods the dairy cows were restricted to 0.2 ha and the fence was moved uphill every 3 hours, repeating this process four times a day. Cow were equipped with activity sensors for 12 h per day. The whole procedure was repeated 2 times after realizing an equalization cuts and both paddocks, a rest time of 30 days and a random reassignment of paddocks to one of the treatments. The cows showed a difference in terms of the percentage of grazing P=0.0072, being higher with the electric fence (55% of the measurement time). From rising-plate-meter estimates of available biomass along the grazing periods, we calculated despite similar forage allowances (electric fence = 48.06 kg DM/cow/d and continuous = 48.21 DM/cow/d) a higher forage intake was obtained in the electric fence treatment (17.5 kg DM/cow/d) compared the continuous stocking (15.7 kg DM/cow/d) (P=0.006). In terms of milk production animals grazing under the differences electrical fence stocking method tended (P=0.0985) to produce more milk (17.39 kg/d) than those grazing in the continuous system (15.16 kg/d) due to the influence of the slope (P=0.05), while for milk quality the protein content was higher for the electric fence (33.7 g/l) than the continuous method (30.5 g/l) (P=0.039). None of the other milk properties differed between methods (P>0.05)

    [<sup>18</sup>F]fluorination of biorelevant arylboronic acid pinacol ester scaffolds synthesized by convergence techniques

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    Aim: The development of small molecules through convergent multicomponent reactions (MCR) has been boosted during the last decade due to the ability to synthesize, virtually without any side-products, numerous small drug-like molecules with several degrees of structural diversity.(1) The association of positron emission tomography (PET) labeling techniques in line with the “one-pot” development of biologically active compounds has the potential to become relevant not only for the evaluation and characterization of those MCR products through molecular imaging, but also to increase the library of radiotracers available. Therefore, since the [18F]fluorination of arylboronic acid pinacol ester derivatives tolerates electron-poor and electro-rich arenes and various functional groups,(2) the main goal of this research work was to achieve the 18F-radiolabeling of several different molecules synthesized through MCR. Materials and Methods: [18F]Fluorination of boronic acid pinacol esters was first extensively optimized using a benzaldehyde derivative in relation to the ideal amount of Cu(II) catalyst and precursor to be used, as well as the reaction solvent. Radiochemical conversion (RCC) yields were assessed by TLC-SG. The optimized radiolabeling conditions were subsequently applied to several structurally different MCR scaffolds comprising biologically relevant pharmacophores (e.g. β-lactam, morpholine, tetrazole, oxazole) that were synthesized to specifically contain a boronic acid pinacol ester group. Results: Radiolabeling with fluorine-18 was achieved with volumes (800 μl) and activities (≤ 2 GBq) compatible with most radiochemistry techniques and modules. In summary, an increase in the quantities of precursor or Cu(II) catalyst lead to higher conversion yields. An optimal amount of precursor (0.06 mmol) and Cu(OTf)2(py)4 (0.04 mmol) was defined for further reactions, with DMA being a preferential solvent over DMF. RCC yields from 15% to 76%, depending on the scaffold, were reproducibly achieved. Interestingly, it was noticed that the structure of the scaffolds, beyond the arylboronic acid, exerts some influence in the final RCC, with electron-withdrawing groups in the para position apparently enhancing the radiolabeling yield. Conclusion: The developed method with high RCC and reproducibility has the potential to be applied in line with MCR and also has a possibility to be incorporated in a later stage of this convergent “one-pot” synthesis strategy. Further studies are currently ongoing to apply this radiolabeling concept to fluorine-containing approved drugs whose boronic acid pinacol ester precursors can be synthesized through MCR (e.g. atorvastatin)
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