Deep learning has performed well in feature extraction and pattern recognition and has been widely studied in the field of fault diagnosis. However, in practical engineering applications, the lack of sample size limits the potential of deep learning in fault diagnosis. Moreover, in engineering practice, it is usually necessary to obtain multidimensional fault information (such as fault localization and quantification), while current methods mostly only provide single-dimensional information.
View Article and Find Full Text PDFIt is of great significance to evaluate the stress state and mechanical properties of deep rock engineering, by inverting the real-time porosity of rocks. In this study, the triaxial compression tests and real-time ultrasonic velocity tests were conducted on siltstone under different confining pressures. Firstly, a nonlinear model for the evolution of rock ultrasonic velocity with axial strain was proposed, based on the characteristic that the ultrasonic velocity rapidly increases and tends to stabilize.
View Article and Find Full Text PDFGeopolymer is a new type of synthesized aluminosilicate material. Compared with ordinary Portland cement, it has better fire resistance and durability, and is more environmentally friendly. In this paper, a high-strength metakaolin-based geopolymer composite (HMGC) has been developed by utilizing quartz powder and steel fibers.
View Article and Find Full Text PDFA series of novel N-alkyl linkers that connect small-molecule library members with their encoding DNA oligonucleotides has been developed. In comparison with the standard amide linker (usually constructed with oligo-AOP-NH ), the N-alkyl linker is not only more chemically stable, but also provides better structural diversity at the linkage point. Chemical variety in the vicinity of the polyglycol terminus, in particular, could affect binding interactions with the target protein.
View Article and Find Full Text PDFA series of macrocyclic analogues were designed and synthesized based on the cocrystal structure of small molecule plasma kallikrein (pKal) inhibitor, , with the pKal protease domain. This led to the discovery of a potent macrocyclic pKal inhibitor , with an IC of 2 nM for one olefinic isomer and 42.3 nM for the other olefinic isomer.
View Article and Find Full Text PDFGeneralized models of joint surface shapes are the foundation for mechanism studies on the mechanical effects of rock joint surface shapes. Based on extensive field investigations of rock joint surface shapes, generalized models for three level shapes named macroscopic outline, surface undulating shape, and microcosmic roughness were established through statistical analyses of 20,078 rock joint surface profiles. The relative amplitude of profile curves was used as a borderline for the division of different level shapes.
View Article and Find Full Text PDFA series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds for further optimization.
View Article and Find Full Text PDFPurinergic receptor P2X3 has been linked to analgesia in a number of pre-clinical models of pain, and is expressed in the human pain perception pathway. Only few P2X3-selective antagonists have been reported to date. This Letter describes the SAR and in vivo analgesic profile of a novel scaffold of selective P2X3 antagonists.
View Article and Find Full Text PDF2,4-Diaminopyrimidines derivatives were developed as a novel class of SNSR4 antagonists. Structure activity relationship of the diamino pyrimidine core was explored and a tool compound suitable for target validation was identified.
View Article and Find Full Text PDFThis paper presents a formal total synthesis of 3-deoxy-D-manno-2-octulosonic acid (KDO) based on a highly double-stereoselective hetero Diels-Alder reaction between an electron-rich diene and ethyl glyoxylate catalyzed by (Salen)Co(II) complex, a new catalyst for Diels-Alder reactions. A facial specific hydroboration followed by oxidative workup leads to a diol system with the trans-diequatorial arrangement of hydroxyl groups at the C-4 and C-5. Inversion of the configuration of the C-5 hydroxyl group in 12 and then ketal formation afford the desired target diisopropylidene-2-deoxy-KDO methyl ester (18), which can be converted to KDO according to the literature procedure.
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