The difunctionalization of vinylpyridines based on the cyclization strategy remains rare and underdeveloped, in contrast to the well-developed hydrogen functionalization. Current exploration on [4 + 2] cyclization of vinylpyridines mainly relies on extremely high temperatures and the LUMO activation of vinylpyridines using boron trifluoride as a strong Lewis acid. Herein, we established a phosphoric acid-catalyzed [4 + 2] cyclization reaction of 3-vinyl-1H-indoles and 2-vinylpyridines by means of the LUMO/HOMO bifunctional activation model.
View Article and Find Full Text PDFNucleotide-binding oligomerization domain-like receptor pyrin domain containing 3 (NLRP3) constitutes an essential inflammasome sensor protein, pivotal in the orchestration of innate immunity. Given its paramount role, NLRP3 has recently emerged as an enticing therapeutic target for disorders associated with inflammation. In this study, we embarked on the design and synthesis of two series of compounds, endowed with the capacity to induce NLRP3 degradation via autophagy-tethering compounds (ATTECs)-an innovative targeted protein degradation technology.
View Article and Find Full Text PDFYing Yong Sheng Tai Xue Bao
September 2023
The evaluation and optimization of landscape ecological pattern has important implications for the accurate improvement of forest quality and high-quality urban development in the Pearl River Delta urban agglomeration. Based on the "one map" data and digital elevation model data of forest resource management in 2021, we evaluated and optimized landscape ecological pattern of the Pearl River Delta urban agglomeration by morphological spatial pattern analysis and minimum cumulative resistance model. The results showed that there were 435861 patches in the Pearl River Delta urban agglomeration that could be used as ecological source area, covering an area of 7346.
View Article and Find Full Text PDFOxygen glucose deprivation-reoxygenation (OGD-R) causes the production of reactive oxygen species (ROS) and oxidative injury in neuronal cells. We tested the potential neuroprotective function of compound 13 (C13), a novel AMP-activated protein kinase (AMPK) activator, against OGD-R. We show that C13 pretreatment protected SH-SY5Y neuronal cells and primary hippocampal neurons from OGD-R.
View Article and Find Full Text PDFObjective: Dehydration on admission is correlated with neurological deterioration (ND). The primary objective of our study was to use support vector machine (SVM) algorithms to identify an ND prognostic model, based on dehydration equations.
Methods: This study included a total of 382 patients hospitalized with acute ischemic stroke.
PI3K-AKT-mTOR signaling is a valuable treatment target for human glioma. LY3023414 is a novel, highly-potent and pan PI3K-AKT-mTOR inhibitor. Here, we show that LY3023414 efficiently inhibited survival and proliferation of primary and established human glioma cells.
View Article and Find Full Text PDFDesminopathies caused by the mutation in the gene coding for desmin are genetically protein aggregation myopathies. Mitochondrial dysfunction is one of pathological changes in the desminopathies at the earliest stage. The molecular mechanisms of mitochondria dysfunction in desminopathies remain exclusive.
View Article and Find Full Text PDFBackground And Purpose: Recovery after stroke varies considerably between individuals. An abundance of evidence suggests that genetic factors contribute to stroke recovery. The aim of this study was to determine whether or not the BDNF G196A polymorphism independently influences the occurrence, severity, and 90-day functional outcome in Chinese patients with ischemic stroke (IS).
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