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关键词： Biologically active molecules   Cyclic-1,3-diketones   Heterocyclic compounds   Michael addition   Styrylisoxazole derivatives  

摘要： A facile synthesis of styrylisoxazole derivatives via Michael addition reaction of 3-methyl-4-nitro-5-styrylisoxazoles to cyclic-1,3-diketones were reported. This method has several additional advantages such as simple operation, mild reaction conditions, broad substrate scope, good functional group tolerance, very good yields without column purification and gram scale synthesis.

关键词： Backscattering coefficient   Elastic scattering   Inelastic scattering   Low energy protons   Plasma-wall interaction   Proton backscattering   Stopping power  

摘要： In a wide range of applications involving proton–solid interaction, including surface analysis, plasma–wall interaction modeling, and proton transport simulations, reliable values of proton backscattering coefficients from solid targets are required. In the energy range from 1 keV to 50 keV, proton backscattering is governed by the combined effects of elastic nuclear scattering and electronic stopping, which must be treated consistently to obtain quantitative results.

关键词： Preterm   Early motor repertoire   General movements optimality   GMOS-R   Motor development  

摘要： To investigate the relationship between early motor repertoire, assessed using the General Movements Optimality Score – Revised (GMOS-R), and motor outcomes at 1, 2 and 5-years' corrected age (CA) in infants born <30 weeks' gestation.

关键词： PINCH-1   Cancer-associated fibroblast   Pancreatic cancer   Matrix   Collagen I  

摘要： Cancer-associated fibroblasts (CAFs) are vital in advancing pancreatic ductal adenocarcinoma (PDAC) cancer growth and fibrosis. Although their roles are recognized, the precise molecular mechanisms remain incompletely understood. The study focuses on PINCH-1, a molecule elevated in various tumors, and its lesser-known effects on tumor stromal cells. This work reveals that PINCH-1 ablation in pancreatic CAFs (P-CAFs) significantly reduces extracellular matrix (ECM) expression, particularly collagen I and fibronectin. For collagen I, this effect is due to PINCH-1's ability to stabilize Notch1 protein, preventing Notch1 degradation, which is crucial for collagen I production. Reintroducing PINCH-1 can reverse collagen I reduction, highlighting a novel mechanism for matrix remodeling through the PINCH-1-Notch1 axis. Moreover, PINCH-1 also boosts cancer cell proliferation via the AKT signaling pathway, as demonstrated in both in vitro and in vivo experiments. We identify PINCH-1 as a master regulator within P-CAFs that promotes PDAC progression through dual mechanisms: (1) sustaining desmoplasia via Notch1-dependent collagen I production and (2) fueling cancer cell proliferation via AKT activation. Targeting the PINCH-1/Notch1/AKT axis presents a novel theragnostic strategy to simultaneously disrupt the fibrotic tumor microenvironment and inhibit tumor growth in PDAC. (188 words)

关键词： Disease-modifying osteoarthritis drugs (DMOADs)   GLP-1 receptor agonists   Immunomodulation   Intra-articular therapy   Liraglutide   Osteoarthritis   Synovial fibrosis   Synovial inflammation  

关键词： Carbonyl diimidazole   CDI   Carboxyl group activator   Carbonyl donor   Amidation   Peptide bond formation  

摘要： 1,1′-Carbonyldiimidazole is one of the most widely used reagents for the activation of carboxylic acid groups. The activated carboxylic acid groups are transformed into a wide range of functional groups. It includes amides, esters, aldehydes, hydroxamic acids, and imides. In addition, it also serves as a carbonyl donor, a dehydrating agent, a decarboxylating agent, an imidazole donor, and a hydroxyl group activator. In this review, the synthetic applications (from 1960 to 2025) of carbonyldiimidazole in organic synthesis are described, and the possible mechanisms involved in the chemical transformations are discussed, wherever applicable.

关键词： Katritzky salt   Imidazo[1,2-a ]pyridine   Photoalkylation   EDA complex  

摘要： The use of visible light-driven photochemical reactions has become increasingly frequent in organic synthesis, as it usually allows for good selectivity, safety and mild reaction conditions. Unfortunately, most organic systems do not absorb visible light, requiring the addition of a photocatalyst or the formation of an Electron Donor-Acceptor (EDA) complex as a way of activating the system. The formation of EDA complexes alters the region in which the organic compounds absorb, making it possible for them to be activated by visible light. In the present study, we explored the C3-alkylation of 2-aryllimidazo[1,2-a]pyridine derivatives in the presence of Katritzky salts and morpholine under visible light. Optimization of the reaction conditions was conducted, achieving 69% yield for C3-alkylated product, and substrate scope valuation afforded 14 examples with up to 96% yield. Among the compounds obtained is a known precursor of Zolpidem, a sedative-hypnotic drug, so this protocol may represent an alternative synthesis for this important pharmaceutical.

关键词： Fear conditioning   Interleukin-1 receptor-1   Microglia   Neuroinflammation   Neuron   Single nuclei RNA-seq   Traumatic brain injury  

摘要： Traumatic brain injury (TBI) increases the risk of developing neuropsychiatric illness and cognitive impairment. Previous work indicates that inflammatory pathways associated with interleukin (IL)-1 and interferon signaling persist in the brain chronically after TBI. Several cell types in the brain express the interleukin-1 receptor-1 (IL-1R1) including endothelia, astrocytes, and neurons. Therefore, the purpose of this study was to determine if IL-1R1-mediated signaling after TBI promotes neuroinflammation and disrupts neuronal homeostasis and cognition. Here, male and female wild-type and global IL-1R1 knock-out (KO) mice were used. Mice were subjected to a diffuse TBI induced by midline fluid percussion injury and several parameters were assessed 3, 7, and 30 days post injury (dpi). At 3 dpi, TBI increased gliosis, cortical inflammation, and the accumulation of leukocytes in the cortex. TBI-associated increase in leukocytes in the brain and neurofilament light chain (NfL) in the plasma 3 dpi were reduced by IL1R1^KO. At 7 dpi, TBI increased gliosis in the cortex and hippocampus that was independent of IL-1R1. IL1R1^KO reduced the TBI associated increases in Il1b, Tnfa, and Irf7 mRNA in the hippocampus and cortex. Moreover, TBI reduced cued fear memory 7 dpi and increased NfL in the plasma. Both deficits were attenuated by IL1R1^KO. IL-1R1 tdTomato reporter mice confirmed that IL-1R1 was expressed in the dentate gyrus and increased by TBI 7 dpi. Next, snRNA-seq studies demonstrated a robust influence of TBI on RNA profiles in the dentate gyrus (DG) and CA1 of the hippocampus 7 dpi. The CA1 and DG had 2572 and 1012 differentially expressed genes (DEGs) influenced by TBI, respectively. Of these DEGs, the majority were decreased after TBI with 73 and 96% prevented in the CA1 and DG by IL1R1^KO. These DEGs were associated with pathways for learning and memory, T-cell signaling, and synapse organization and main

关键词： Crystallization   D-J equivalence   Polytope   Regular genus   Small cover   Z2n-action  

摘要： A crystallization of a PL manifold is an edge-colored graph that corresponds to a contracted triangulation of the manifold, facilitating the study of its topological and combinatorial properties. A small cover over a simple n-polytope $P^n$ is a closed n-manifold with a locally standard ${\mathbb{Z}}_2^n$-action such that its orbit space is homeomorphic to $P^n$. In this article, we study the crystallizations of small covers over the n-simplex ${\mathrm{\Delta }}^n$ and the prism ${\mathrm{\Delta }}^{n-1}\times I$. It is known that the small cover over the n-simplex ${\mathrm{\Delta }}^n$ is ${\mathbb{RP}}^n$. For every $n\ge 2$, we prove that