The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors

Cyclic urea SD146, a potent HIV protease inhibitor bearing a flat resistance profile, possessed poor solubility and bioavailability, which precluded further development of the compound. In an effort to improve upon the pharmacokinetic profile of the compound, several analogs modified at the P1/P1' residues were prepared and evaluated. Several of those compounds displayed significant improvement of physical properties.     

Breakfasts high in monoglyceride or triglyceride: no differential effect on appetite or energy intake

OBJECTIVE: To test whether isoenergetic isoenergetically-dense doses of dietary 1-monoglyceride or triglyceride differentially influence appetite and meal-to-meal energy intake in man. DESIGN: Six men and six women were each studied twice in a 2 d protocol. On day 1 (maintenance day) they were fed a medium fat (MF) maintenance diet (MF: 40% fat, 47% carbohydrate and 13% protein by energy) calculated at 1.6 x resting metabolic rate (RMR). On day 2 (manipulation day) at 08.30 h subjects consumed a high-fat breakfast designed to contain 80-85% of RMR, composition 10% protein, 56% fat and 34% carbohydrate by energy, with 65% of energy for fat derived as either 1-monoglyceride or triglyceride. Food and energy intake were monitored at lunch (given at 12.30pm) and throughout the remainder of the day. During this time subjects had ad libitum access to isoenergetic, isoenergetically dense MF (40:47:13) foods (550kJ/100g), until 22.30pm). Subjective hunger and satiety were tracked hourly, during waking hours. RESULTS: There was no significant effect of fat type on food or energy intake at lunch or during the ad libitum period. There was no diet effect on subjective hunger (F(1,10)0.00; P= 0.975) in the inter-meal periods of morning or afternoon, nor during the whole day. Subjects found both diets to be similarly pleasant (F(1,61)0.84;P= 0.364). Men and women responded similarly, except that men ate more on all occasions than women. CONCLUSIONS: This study suggests that when a large dose of l-monoglyceride or triglyceride is incorporated into a breakfast meal, it behaves in a manner that is very similar to triglyceride in terms of the effects on hunger, appetite or feeding behaviour.     

Unsupervised Scale-Consistent Depth Learning from Video

International Journal of Computer Vision - We propose a monocular depth estimation method SC-Depth, which requires only unlabelled videos for training and enables the scale-consistent...     

Regressing Local to Global Shape Properties for Online Segmentation and Tracking

We propose a novel regression based framework that uses online learned shape information to reconstruct occluded object contours. Our key insight is to regress the global, coarse, properties of shape from its local properties, i.e. its details. We do this by representing shapes using their 2D discrete cosine transforms and by regressing low frequency from high frequency harmonics. We learn this regression model using Locally Weighted Projection Regression which expedites online, incremental learning. After sufficient observation of a set of unoccluded shapes, the learned model can detect occlusion and recover the full shapes from the occluded ones. We demonstrate the ideas using a level-set based tracking system that provides shape and pose, however, the framework could be embedded in any segmentation-based tracking system. Our experiments demonstrate the efficacy of the method on a variety of objects using both real data and artificial data.     

Preparation and characterization of trilobal activated carbon fibers

The objective of this research was to evaluate the effectiveness of several different methods for controlling the pore size and pore size distribution in activated carbon fibers. Variables studied included fiber shape, activation time, and the addition of small amounts of silver nitrate. Pure isotropic pitch and the same isotropic pitch containing 1 wt.% silver were melt spun to form fibers with round and trilobal cross sections. These fibers were then stabilized, carbonized, and activated in carbon dioxide. Field emission scanning electron microscopy (FE SEM), electron dispersive spectra (EDS), and wavelength dispersive spectra (WDS) were used to monitor the size and distribution of the silver particles in the fibers before and after activation. Each of these analyses showed that the distribution of silver particles was extremely uniform before and after activation. The fibers were also weighed before and after activation to determine the percent burn-off. The BET specific surface areas of the activated fibers were determined from N₂ adsorption isotherms measured at −196 °C. The results showed that round and trilobal fibers with equivalent cross-sectional areas yielded similar burn-off values and specific surface areas after activation. Also, activation rates were found to be independent of CO₂ flow rate. The porosity of the activated fibers depended on the total time of activation and the cross-sectional area of fibers. The N₂ adsorption measurements showed that the activated fibers had extremely high specific surface areas (greater than 3000 m²/g) and high degrees of meso- and macro-porosity. FE SEM was also used to investigate surface texture and size of pore openings on the surfaces of the activated fibers. The photos showed that silver particles generated surface macro- and mesopores, in agreement with the inferences from N₂ adsorption measurements.     

Synthesis,structure, and characterization of the thorium zirconolite CaZr1-xThxTi2O7 system

A series of zirconolite ceramics with composition CaZr_1-xTh_xTi₂O₇ (Δx = 0.10) were reactively sintered at 1350°C for 20 h, in air (0 ≤ x ≤ 0.60) and 5% H₂/N₂ (0 ≤ x ≤ 0.40). A sample with composition corresponding to x = 0.20 was also produced by hot isostatic pressing (HIP) at 1300°C and 100 MPa for 4 hours. Th⁴⁺ immobilization was most readily achieved under oxidizing conditions, with Th⁴⁺ preferentially incorporated within a pyrochlore-structured phase in the range 0.10 ≤ x ≤ 0.50, yet formation of the zirconolite-4M polytype was not observed. We report the novel synthesis of single-phase pyrochlore with nominal composition CaZr_0.40Th_0.60Ti₂O₇ when targeting x = 0.60. Th⁴⁺ incorporation under reducing conditions produced a secondary Th-bearing perovskite, comprising 24.2 ± 0.6 wt% of the phase assemblage when targeting x = 0.40, alongside 8.8 ± 0.3 wt% undigested ThO₂. Under reducing conditions, powder XRD data were consistent with zirconolite adopting the 3T polytype structure. The sample produced by HIP presented a nonequilibrium phase assemblage, yielding a major phase of zirconolite-2M alongside accessory Th⁴⁺-bearing phases ThTi₂O₆, ThO₂, and perovskite. These data highlight the efficacy of Th⁴⁺ as a Pu⁴⁺ surrogate, with implications for the formation of Zr-stabilized Th-pyrochlore phases as matrices for waste with elevated Th⁴⁺ content.     

Ongoing verification of a multiphysics community code: FLASH

When developing a complex, multi‐authored code, daily testing on multiple platforms and under a variety of conditions is essential. It is therefore necessary to have a regression test suite that is easily administered and configured, as well as a way to easily view and interpret the test suite results. We describe the methodology for verification of FLASH, a highly capable multiphysics scientific application code with a wide user base. The methodology uses a combination of unit and regression tests and an in‐house testing software that is optimized for operation under limited resources. Although our practical implementations do not always comply with theoretical regression‐testing research, our methodology provides a comprehensive verification of a large scientific code under resource constraints.Copyright © 2013 John Wiley & Sons, Ltd.     

Evaluating and improving the effectiveness and efficiency of design process communication

Project information management research enables the efficient exchange of information, but does not effectively communicate process. Design process management research effectively communicates processes, but with methods too inefficient to be adopted in practice. The lack of methods for effective and efficient design process communication manifests as a struggle for Architecture, Engineering, and Construction industry professionals to: (1) collaborate within projects, (2) share processes between projects, and (3) understand processes across projects to strategically invest in improvement. These struggles motivate the paper’s first contribution: a research method for evaluating a design management methodology’s ability to effectively and efficiently communicate design processes. As a second contribution, this paper validates the Design Process Communication Methodology (DPCM). DPCM specifies elements and methods for exchanging and organizing digital information to support knowledge-intensive design processes. Cloud computing enables the operationalization of DPCM as a tool that enables interaction with a project’s information. Results from this operationalization demonstrate that designers employing DPCM accurately capture processes with little effort. When collaborating, improved process clarity and information consistency result in less rework, and positive iteration enables increased consideration of multi-disciplinary design trends. Designers share processes between project teams with fewer process mistakes. DPCM enables the understanding of processes providing more insights into the relationships between design integration and project performance; and more opportunities for strategic investment in improved processes.