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Divyaraj Puthran Boja Poojary Soukhyarani G. Nayak Nikil Purushotham Manjunath Bhat Hemant Hedge 《中国化学会会志》2020,67(7):1278-1288
2-amino-5-(3-fluoro-4-methoxyphenyl)thiophene-3-carbonitrile derivatives have been synthesized from 1-(3-fluoro-4-methoxyphenyl)ethanone, malononitrile, mild base, and sulfur powder using the Gewald method through a multistep reaction sequence. The structures of newly synthesized compounds were established on the basis of their elemental analyses, IR, 1H NMR, 13C NMR, and mass spectral data, and then synthesized compounds were screened for their in vitro antimicrobial activity. Among them, derivatives 3b (thiphene), 3f (pyrazole), and 3d (halogen) showed good activity and remaining derivatives exhibited moderate activity. 相似文献
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Tsann-Shyong Liu Nikil Jayant 《IEEE transactions on image processing》1995,4(7):1032-1035
A new adaptive postprocessing algorithm to enhance the quality of a noisy video sequence is presented. The algorithm recognizes that the visibility of noise depends on local signal characteristics. It therefore classifies the video signal into different classes and uses separate nonlinear filters matched to each class. The most general version of the algorithm employs motion-compensated frame averaging to improve picture quality in a first stage. A classification algorithm subsequently divides subblocks of pixels in the averaged frame into four classes: edge, smooth, nonsmooth with motion and nonsmooth without motion. Spatial algorithms that perform multilevel median filtering, double median filtering, and median filtering are used for pixels belonging to edge, smooth, and nonsmooth with motion categories. Pixels in the nonsmooth, unmoving category are left unfiltered to preserve corresponding image texture. In a simpler version of this four-class system, the motion cues and motion-compensated frame averaging are eliminated, and the purely spatial filtering is based on a three-class algorithm. When used at the output of a 3-D subband coder at 384 kbps, the spatial postfilter was shown to provide a consistent gain in subjectively evaluated picture quality. Twenty-five viewers participated in an experiment involving three coded sequences. In a pairwise comparison of postfiltered and unfiltered sequences, the postfiltered version was judged to be better in 63 out of 75 instances. 相似文献
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Highly Productive Oxidative Biocatalysis in Continuous Flow by Enhancing the Aqueous Equilibrium Solubility of Oxygen 下载免费PDF全文
Dr. Michael R. Chapman Dr. Sebastian C. Cosgrove Prof. Nicholas J. Turner Prof. Nikil Kapur Prof. A. John Blacker 《Angewandte Chemie (International ed. in English)》2018,57(33):10535-10539
We report a simple, mild, and synthetically clean approach to accelerate the rate of enzymatic oxidation reactions by a factor of up to 100 when compared to conventional batch gas/liquid systems. Biocatalytic decomposition of H2O2 is used to produce a soluble source of O2 directly in reaction media, thereby enabling the concentration of aqueous O2 to be increased beyond equilibrium solubility under safe and practical conditions. To best exploit this method, a novel flow reactor was developed to maximize productivity (g product L?1 h?1). This scalable benchtop method provides a distinct advantage over conventional bio‐oxidation in that no pressurized gas or specialist equipment is employed. The method is general across different oxidase enzymes and compatible with a variety of functional groups. These results culminate in record space‐time yields for bio‐oxidation. 相似文献
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Methods that can screen large databases to retrieve a structurally diverse set of compounds with desirable bioactivity properties are critical in the drug discovery and development process. This paper presents a set of such methods that are designed to find compounds that are structurally different to a certain query compound while retaining its bioactivity properties (scaffold hops). These methods utilize various indirect ways of measuring the similarity between the query and a compound that take into account additional information beyond their structure-based similarities. The set of techniques that are presented capture these indirect similarities using approaches based on analyzing the similarity network formed by the query and the database compounds. Experimental evaluation shows that most of these methods substantially outperform previously developed approaches both in terms of their ability to identify structurally diverse active compounds as well as active compounds in general. 相似文献
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Nejatollahi Hamid Shahhosseini Sina Cammarota Rosario Dutt Nikil 《Journal of Signal Processing Systems》2021,93(10):1139-1148
Journal of Signal Processing Systems - Quantum computers are imminent threat to secure signal processing because they can break the contemporary public-key cryptography schemes in polynomial time.... 相似文献
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Adam D. Clayton Edward O. Pyzer-Knapp Mark Purdie Martin F. Jones Alexandre Barthelme John Pavey Nikil Kapur Thomas W. Chamberlain A. John Blacker Richard A. Bourne 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2023,135(3):e202214511
The optimization of multistep chemical syntheses is critical for the rapid development of new pharmaceuticals. However, concatenating individually optimized reactions can lead to inefficient multistep syntheses, owing to chemical interdependencies between the steps. Herein, we develop an automated continuous flow platform for the simultaneous optimization of telescoped reactions. Our approach is applied to a Heck cyclization-deprotection reaction sequence, used in the synthesis of a precursor for 1-methyltetrahydroisoquinoline C5 functionalization. A simple method for multipoint sampling with a single online HPLC instrument was designed, enabling accurate quantification of each reaction, and an in-depth understanding of the reaction pathways. Notably, integration of Bayesian optimization techniques identified an 81 % overall yield in just 14 h, and revealed a favorable competing pathway for formation of the desired product. 相似文献
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Mark A. Levenstein Clara Anduix‐Canto Yi‐Yeoun Kim Mark A. Holden Carlos Gonzlez Nio David C. Green Stephanie E. Foster Alexander N. Kulak Lata Govada Naomi E. Chayen Sarah J. Day Chiu C. Tang Britta Weinhausen Manfred Burghammer Nikil Kapur Fiona C. Meldrum 《Advanced functional materials》2019,29(19)
The ability to control crystallization reactions is required in a vast range of processes including the production of functional inorganic materials and pharmaceuticals and the prevention of scale. However, it is currently limited by a lack of understanding of the mechanisms underlying crystal nucleation and growth. To address this challenge, it is necessary to carry out crystallization reactions in well‐defined environments, and ideally to perform in situ measurements. Here, a versatile microfluidic synchrotron‐based technique is presented to meet these demands. Droplet microfluidic‐coupled X‐ray diffraction (DMC‐XRD) enables the collection of time‐resolved, serial diffraction patterns from a stream of flowing droplets containing growing crystals. The droplets offer reproducible reaction environments, and radiation damage is effectively eliminated by the short residence time of each droplet in the beam. DMC‐XRD is then used to identify effective particulate nucleating agents for calcium carbonate and to study their influence on the crystallization pathway. Bioactive glasses and a model material for mineral dust are shown to significantly lower the induction time, highlighting the importance of both surface chemistry and topography on the nucleating efficiency of a surface. This technology is also extremely versatile, and could be used to study dynamic reactions with a wide range of synchrotron‐based techniques. 相似文献
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The title compound, C22H23N2BrO2 was synthesized via one-pot reductive cyclization method and characterized by CNH analysis, FT-IR, UV-visible, mass, 1H and 13C NMR spectra, thermogravimetric analysis (TGA) and single crystal X-ray diffraction method. The compound crystallizes in monoclinic crystal system: sp. gr. P21/c, Z = 4. The crystal data reveals that the intermolecular interactions of the C–H···π and π···π type connect the molecules which was also visualized with the help of Hirshfeld surface analysis. 相似文献
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Virtualizing on-chip distributed ScratchPad memories for low power and trusted application execution
Luis Angel D. Bathen Dongyun Shin Sung-Soo Lim Nikil D. Dutt 《Design Automation for Embedded Systems》2013,17(2):377-409
Emerging multicore platforms are increasingly deploying distributed scratchpad memories to achieve lower energy and area together with higher predictability; but this requires transparent and efficient software management of these critical resources. In this paper, we introduce the concept of ScratchPad Memory virtualization, a hardware/software run-time layer (called SPMVisor) that virtualizes the scratchpad memory space in order to facilitate the use of distributed SPMs in an efficient, transparent and secure manner. We introduce the notion of virtual scratchpad memories (vSPMs), which can be dynamically created and managed as regular SPMs. The SPMVisor exploits policy-driven allocation strategies based on application privilege levels and data level prioritization metrics (e.g., utilization) to efficiently manage the on-chip memory real-estate. Our experimental results on Mediabench/CHStone benchmarks running on various Chip-Multiprocessor configurations and software stacks (RTOS, virtualization, secure execution) showed that SPMVisor enhances performance by 71 % on average and reduces power consumption by 79 % on average with respect to traditional context switching schemes. We showed the benefits of using vSPMs in a various environments (a RTOS multi-tasking environment, a virtualization environment, and a trusted execution environment). Furthermore, we explored the effects of mapping instructions and data onto vSPMs, and showed that sharing on-chip space reduces both execution time and energy by an average 16 % and 12 % respectively. We then compared our priority-driven memory allocation scheme with traditional dynamic allocation and showed an average 54 % execution time reduction and 65 % energy savings. Finally, to further validate the SPMVisor’s benefits, we modified the initial bus-based architecture to include a mesh-based CMP with up to 4×4 nodes. We were able to observe that SPMVisor’s priority-driven allocator was able to reduce execution time by an average 17 % with respect to competing allocation policies, while saving an average 65 % across various architectural configurations. We were also able to observe that SPMVisor reduces execution time by an average 12.6 % with respect to competing allocation policies, while saving an average 63.5 % in total energy for various architectural configuration running 1024 jobs. 相似文献