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排序方式: 共有761条查询结果,搜索用时 16 毫秒
751.
Dr. Bianca Schulte Maria König Prof. Dr. Beate I. Escher Sophie Wittenburg Matic Proj Valentina Wolf Carina Lemke Dr. Gregor Schnakenburg Prof. Dr. Izidor Sosič Prof. Dr. Hendrik Streeck Prof. Dr. Christa E. Müller Prof. Dr. Michael Gütschow Dr. Christian Steinebach 《ChemMedChem》2022,17(5):e202100732
Naturally occurring compounds represent a vast pool of pharmacologically active entities. One of such compounds is andrographolide, which is endowed with many beneficial properties, including the activity against severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2). To initiate a drug repurposing or hit optimization campaign, it is imperative to unravel the primary mechanism(s) of the antiviral action of andrographolide. Here, we showed by means of a reporter gene assay that andrographolide exerts its anti-SARS-CoV-2 effects by inhibiting the interaction between Kelch-like ECH-associated protein 1 (KEAP1) and nuclear factor erythroid 2-related factor 2 (NRF2) causing NRF2 upregulation. Moreover, we demonstrated that subtle structural modifications of andrographolide could lead to derivatives with stronger on-target activities and improved physicochemical properties. Our results indicate that further optimization of this structural class is warranted to develop novel COVID-19 therapies. 相似文献
752.
753.
Eilien Heinrich Olga Hartwig Christine Walt Arefeh Kardani Marcus Koch Leila Pourtalebi Jahromi Jessica Hoppstädter Alexandra K. Kiemer Brigitta Loretz Claus-Michael Lehr Gregor Fuhrmann 《Small (Weinheim an der Bergstrasse, Germany)》2023,19(25):2207479
Recently, extracellular vesicles (EVs) sparked substantial therapeutic interest, particularly due to their ability to mediate targeted transport between tissues and cells. Yet, EVs’ technological translation as therapeutics strongly depends on better biocompatibility assessments in more complex models and elementary in vitro–in vivo correlation, and comparison of mammalian versus bacterial vesicles. With this in mind, two new types of EVs derived from human B-lymphoid cells with low immunogenicity and from non-pathogenic myxobacteria SBSr073 are introduced here. A large-scale isolation protocol to reduce plastic waste and cultivation space toward sustainable EV research is established. The biocompatibility of mammalian and bacterial EVs is comprehensively evaluated using cytokine release and endotoxin assays in vitro, and an in vivo zebrafish larvae model is applied. A complex three-dimensional human cell culture model is used to understand the spatial distribution of vesicles in epithelial and immune cells and again used zebrafish larvae to study the biodistribution in vivo. Finally, vesicles are successfully loaded with the fluoroquinolone ciprofloxacin (CPX) and showed lower toxicity in zebrafish larvae than free CPX. The loaded vesicles are then tested effectively on enteropathogenic Shigella, whose infections are currently showing increasing resistance against available antibiotics. 相似文献
754.
Yigitbas Enes Gorissen Simon Weidmann Nils Engels Gregor 《Software and Systems Modeling》2023,22(5):1397-1425
Software and Systems Modeling - Modeling is a key activity in conceptual design and system design. Through collaborative modeling, end-users, stakeholders, experts, and entrepreneurs are able to... 相似文献
755.
Ginu R. George Marina Bockelmann Leonhard Schmalhorst Didier Beton Alexandra Gerstle Lars Torkuhl Andreas Lindermeir Gregor D. Wehinger 《American Institute of Chemical Engineers》2023,69(1):e17284
In recent years, the catalyst pellets made of open-cell metallic foams have been identified as a promising alternative in fixed-bed reactors. A reliable modeling tool is necessary to investigate the suitability of different foam properties and the shapes of foam pellets. In this article, a workflow for a detailed computational fluid dynamics (CFD) model is presented, which aims to study the flow characteristics in the slender packed beds made of metal foam pellets. The CFD model accounts for the actual random packing structure and the fluid flow throughout the interstitial regions is fully resolved, whereas flow through the porous foam pellets is represented by the closure equations for the porous media model. The bed structure is generated using rigid body dynamics (RBD) and the influence of the catalyst loading method is also considered. The mean bed voidage and the pressure drop predicted by the simulations show good agreement with the experimental data. 相似文献
756.
Prof. Dr. Jeroen S. Dickschat Dr. Zhiyang Quan Dr. Gregor Schnakenburg 《Chembiochem : a European journal of chemical biology》2023,24(23):e202300581
A terpene synthase from Nonomuraea coxensis was identified as (+)-1-epi-cubenol synthase. The enzyme is phylogenetically unrelated to the known enzyme of the same function that is widespread in streptomycetes. Isotopic labelling experiments were performed to unambiguously assign the NMR data and to investigate hydrogen migrations during terpene cyclisations. Epoxidations of (+)-1-epi-cubenol and of the plant derived compounds (−)-cubenol and (−)-1-epi-cubenol confirmed the structure of a natural product isolated from the brown alga Dictyopteris divaricata and allowed to conclude on its absolute configuration. The crystal structures of the epoxides from (+)- and (−)-1-epi-cubenol and the acid catalysed conversion into an isomeric ketone are reported. 相似文献
757.
758.
Sebastian Simon Marko Bertmer Gregor J. G. Gluth 《International Journal of Applied Ceramic Technology》2022,19(6):3179-3190
Hydrous lithium aluminosilicate (L–A–S–H) and lithium aluminate (L–A–H) gels are candidate precursors for glass-ceramics and ceramics with potential advantages over conventional processing routes. However, their structure before calcination remained largely unknown, despite the importance of precursor structure on the properties of the resulting materials. In the present study, it is demonstrated that L–A–S–H and L–A–H gels with Li/Al ≤ 1 can be produced via an organic steric entrapment route, while higher Li/Al ratios lead to crystallization of gibbsite or nordstrandite. The composition and the structure of the gels was studied by thermogravimetric analysis, X-ray diffraction, 27Al and 29Si magic-angle spinning nuclear magnetic resonance, and Raman spectroscopy. Aluminium was found to be almost exclusively in six-fold coordination in both the L–A–H and the L–A–S–H gels. Silicon in the L–A–S–H gels was mainly in Q4 sites and to a lesser extent in Q3 sites (four-fold coordination with no Si–O–Al bonds). The results thus indicate that silica-rich and aluminium-rich domains formed in these gels. 相似文献
759.
Herwig Prasch Dr. Andreas Wolfsgruber Dr. Martin Thonhofer André Culum Christoph Mandl Dr. Patrick Weber Melanie Zündel Dr. Seyed A. Nasseri Dr. Andres Gonzalez Santana Dr. Gregor Tegl Prof. Dr. Bernd Nidetzky Prof. Dr. Karl Gruber Prof. Dr. Arnold E. Stütz Prof. Dr. Stephen G. Withers Prof. Dr. Tanja M. Wrodnigg 《Chembiochem : a European journal of chemical biology》2023,24(23):e202300480
Selective covalent labelling of enzymes using small molecule probes has advanced the scopes of protein profiling. The covalent bond formation to a specific target is the key step of activity-based protein profiling (ABPP), a method which has become an indispensable tool for measuring enzyme activity in complex matrices. With respect to carbohydrate processing enzymes, strategies for ABPP so far involve labelling the active site of the enzyme, which results in permanent loss of activity. Here, we report in a proof of concept study the use of ligand-directed chemistry (LDC) for labelling glycoside hydrolases near – but not in – the active site. During the labelling process, the competitive inhibitor is cleaved from the probe, departs the active site and the enzyme maintains its catalytic activity. To this end, we designed a building block synthetic concept for small molecule probes containing iminosugar-based reversible inhibitors for labelling of two model β-glucosidases. The results indicate that the LDC approach can be adaptable for covalent proximity labelling of glycoside hydrolases. 相似文献
760.
Darina Makov Ivan Kov
ik Gregor Ondrejovi
《Advanced Synthesis \u0026amp; Catalysis》1991,333(3):389-396
By replacement of methanol in the Cu4OX6(MeOH)4 (X Cl, Br) complexes with thiourea (tu), N,N′-diphenylthiourea (diftu), N,N′-dimethlthiourea (dimtu), tetramethylthiourea (tmtu) and acetylthiourea (actu), the complexes Cu4OCl6L4 where L tu, tu(0.3 Et2O), diftu, dimtu, tmtu, actu (0.5Et2O) and the complexes Cu4OBr6L4, where L tu, diftu, dimtu, tmtu have been prepared. Their infrared and electronic spectra indicate the presence of Cu4O grouping and the trigonal bipyramidal coordination of copper(II). These complexes exhibit e.p.r. signals in the temperature range 100–260 K, in contrast to other known complexes of this structural type, which showed the e.p.r. signals at significantly lower temperatures. Thiourea and its derivatives are not able to reduce copper(II) in reaction with the tetranuclear Cu4OX6(MeOH)4 complexes in methanol-ether solution due to the redox stabilizing effect of the tetranuclear structure. 相似文献