61 research outputs found

    A Pervasive Computational Intelligence based Cognitive Security Co-design Framework for Hype-connected Embedded Industrial IoT

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    The amplified connectivity of routine IoT entities can expose various security trajectories for cybercriminals to execute malevolent attacks. These dangers are even amplified by the source limitations and heterogeneity of low-budget IoT/IIoT nodes, which create existing multitude-centered and fixed perimeter-oriented security tools inappropriate for vibrant IoT settings. The offered emulation assessment exemplifies the remunerations of implementing context aware co-design oriented cognitive security method in assimilated IIoT settings and delivers exciting understandings in the strategy execution to drive forthcoming study. The innovative features of our system is in its capability to get by with irregular system connectivity as well as node limitations in terms of scares computational ability, limited buffer (at edge node), and finite energy. Based on real-time analytical data, projected scheme select the paramount probable end-to-end security system possibility that ties with an agreed set of node constraints. The paper achieves its goals by recognizing some gaps in the security explicit to node subclass that is vital to our system’s operations

    Synthesis, Biodistribution and In vitro Evaluation of Brain Permeable High Affinity Type 2 Cannabinoid Receptor Agonists [11C]MA2 and [18F]MA3

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    Abstract The type 2 cannabinoid receptor (CB2) is a member of the endocannabinoid system and is known for its important role in (neuro)inflammation. A PET-imaging agent that allows in vivo visualization of CB2 expression may thus allow quantification of neuroinflammation. In this paper, we report the synthesis, radiosynthesis, biodistribution and in vitro evaluation of a carbon-11 ([11C]MA2) and a fluorine-18 ([18F]MA3) labeled analogue of a highly potent N-arylamide oxadiazole CB2 agonist (EC50 = 0.015 nM). MA2 and MA3 behaved as potent CB2 agonist (EC50: 3 nM and 0.1 nM, respectively) and their in vitro binding affinity for hCB2 was found to be 87 nM and 0.8 nM, respectively. Also MA3 (substituted with a fluoro ethyl group) was found to have higher binding affinity and EC50 values when compared to the originally reported trifluoromethyl analogue 12. [11C]MA2 and [18F]MA3 were successfully synthesized with good radiochemical yield, high radiochemical purity and high specific activity. In mice, both tracers were efficiently cleared from blood and all major organs by the hepatobiliary pathway and importantly these compounds showed high brain uptake. In conclusion, [11C]MA2 and [18F]MA3 are shown to be high potent CB2 agonists with good brain uptake, these favorable characteristics makes them potential PET probes for in vivo imaging of brain CB2 receptors. However in view of its higher affinity and selectivity, further detailed evaluation of MA3 as a PET tracer for CB2 is warranted

    Catalytic asymmetric additions of carbon-centered nucleophiles to nitrogen-containing aromatic heterocycles

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    Nearly a century after the first report of the Reissert reaction the first catalytic, asymmetric example was published. Since then there have been a small number of reports of similar reaction types: activation of nitrogen-containing aromatic rings through alkylation or acylation, followed by the addition of a carbon-centered nucleophile to the ring. These reactions place great demands on catalyst design; many of the catalysts are bifunctional, simultaneously activating both nucleophiles and electrophiles. The structures obtained from such reactions may easily be derivatized into natural products or drug-like structures. Despite the elegance of the known examples, there are still many reaction types that have not been reported

    PET imaging with [11C]NMS-E973 reveals difference between healthy and malignant expressed HSP90

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    status: accepte

    Synthetic strategies for radioligands for in vivo imaging of brain cannabinoid type-1 receptors

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    Despite its abundant expression in the brain, the cannabinoid type-1 (CB1) receptor was discovered only in 1988. During the last decade, efforts from several research groups have made it possible to visualize the CB1 receptor in vivo to unravel its role in the brain physiology and pathology. This review discusses strategies for (radio)synthesis of radioligands for in vivo imaging of CB1 receptors

    Novel polyaniline-supported molybdenum-catalyzed aerobic oxidation of alcohols to aldehydes and ketones

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    Oxidation of alcohols to aldehydes and ketones has been studied in high yields using molecular oxygen and a catalytic amount of 1 in toluene under stirring (ca. 100 degrees C). The reactions of primary alcohols are faster compared to secondary alcohols and the catalyst 1 can be recycled without loss of activity
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