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101.
Synthesis and Reactions of Chiral Dithiocarbamates Derived from (R)-(−)- or (S)-(+)-2- The synthesis, diastereoselective alkylation reactions, dithiocarboxylation, and aldol condensation of several substituted methyl (R1 CH2) (S)-2-(methoxymethyl)-pyrrolidine-1-dithiocarboxylates (S)- 2 and of the corresponding (R)-derivatives (R)- 2 are described. The new enantiomeric dithiocarbamates (S) -2a – e , and (R) -2a – d are obtained by reaction of (S)-(+)-[(S) -1 ] or (R)-(−)-2-(methoxymethyl)-pyrrolidine [(R) -1 ], respectively, with carbon disulfide in dry methanol/anhydrous sodium acetate and the appropriate alkylating agent. The cyclic ketene dithioacetals (S) -3 and (R) -3 are formed by dithiocarboxylation procedure of (S) -2a and (R) -2a whereas (S) -6 and (R) -6 are obtained by aldol reaction with isobutyraldehyde. (S)- 2c , d and (R) -2c , d react in a diastereoselective manner after deprotonation with n-BuLi or LiTMP/LiBr at −78°C in THF with alkyl halides to the enantiomeric compounds 4a /ent -4a, 4b /ent -4b and 5 /ent -5 , respectively. 相似文献
102.
Kseniya Khamina Andreas B. Diendorfer Susanna Skalicky Moritz Weigl Marianne Pultar Teresa L. Krammer Catharine Aquino Fournier Amy L. Schofield Carolin Otto Aaron Thomas Smith Nina Buchtele Christian Schoergenhofer Bernd Jilma Bernhard J. H. Frank Jochen G. Hofstaetter Regina Grillari Johannes Grillari Klemens Ruprecht Christopher E. Goldring Hubert Rehrauer Warren E. Glaab Matthias Hackl 《International journal of molecular sciences》2022,23(3)
103.
Dr. Lukas Kröger Dr. Constantin G. Daniliuc Deeba Ensan Sebastian Borgert Dr. Christian Nienberg Miriam Lauwers Dr. Michaela Steinkrüger Prof. Joachim Jose Dr. Markus Pietsch Prof. Bernhard Wünsch 《ChemMedChem》2020,15(10):871-881
The serine/threonine kinase CK2 modulates the activity of more than 300 proteins and thus plays a crucial role in various physiological and pathophysiological processes including neurodegenerative disorders of the central nervous system and cancer. The enzymatic activity of CK2 is controlled by the equilibrium between the heterotetrameric holoenzyme CK2α2β2 and its monomeric subunits CK2α and CK2β. A series of analogues of W16 ((3aR,4S,10S,10aS)-4-{[(S)-4-benzyl-2-oxo-1,3-oxazolidin-3-yl]carbonyl}-10-(3,4,5-trimethoxyphenyl)-4,5,10,10a-tetrahydrofuro[3,4-b]carbazole-1,3(3aH)-dione ((+)- 3 a )) was prepared in an one-pot, three-component Levy reaction. The stereochemistry of the tetracyclic compounds was analyzed. Additionally, the chemically labile anhydride structure of the furocarbazoles 3 was replaced by a more stable imide ( 9 ) and N-methylimide ( 10 ) substructure. The enantiomer (−)- 3 a (Ki=4.9 μM) of the lead compound (+)- 3 a (Ki=31 μM) showed a more than sixfold increased inhibition of the CK2α/CK2β interaction (protein-protein interaction inhibition, PPII) in a microscale thermophoresis (MST) assay. However, (−)- 3 a did not show an increased enzyme inhibition of the CK2α2β2 holoenzyme, the CK2α subunit or the mutated CK2α′ C336S subunit in the capillary electrophoresis assay. In the pyrrolocarbazole series, the imide (−)- 9 a (Ki=3.6 μM) and the N-methylimide (+)- 10 a (Ki=2.8 μM) represent the most promising inhibitors of the CK2α/CK2β interaction. However, neither compound could inhibit enzymatic activity. Unexpectedly, the racemic tetracyclic pyrrolocarbazole (±)- 12 , with a carboxy moiety in the 4-position, displays the highest CK2α/CK2β interaction inhibition (Ki=1.8 μM) of this series of compounds. 相似文献
104.
Aerobic biodegradation of polyethylene glycols of different molecular weights in wastewater and seawater 总被引:1,自引:0,他引:1
In order to distinguish between aerobic biodegradation of synthetic polymers in fresh and seawater, polyethylene glycols (PEGs) were systematically and comparatively investigated in inocula from municipal wastewater and seawater aquarium filters for the first time. The molecular weight (MW) of the PEGs, (HO(CH(2)CH(2)O)(n)H, n=3-1350) as representatives of water-soluble polymers, ranged from 250 to 57,800Da. The biodegradation was observed by removal of dissolved organic carbon and carbon dioxide production by applying standardized ISO and OECD test methods. Specific analyses using liquid chromatography mass spectrometry (LC-MS) and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF-MS) were performed. All PEGs selected were completely biodegradable in freshwater media within 65d. PEGs with an MW up to 14,600Da have a similar degradation pathway which is characterized by gradual splitting of C(2)-units off the chain resulting in formation of short-chain PEGs. In artificial seawater media, full biodegradation of PEGs up to 7400Da required more time than in freshwater. PEGs with MW 10,300 and 14,600Da were only partially degraded whereas PEGs with MW 26,600 and 57,800Da were not degraded for a period of 135d. The biodegradation pathway of PEG 250 and PEG 970 in seawater is similar to that for freshwater. For PEGs having an MW from 2000 to 10,300Da, the degradation pathway in seawater differs from the pathway of the shorter PEGs. 相似文献
105.
Stephan W. Reinhold Thomas Scherl Benjamin Stölcker Tobias Bergler Ute Hoffmann Christian Weingart Miriam C. Banas Dmitrij Kollins Martin C. Kammerl Bernd Krüger Bernhard Kaess Bernhard K. Krämer Bernhard Banas 《Lipids》2013,48(2):167-175
Acute transplant rejection is the leading cause of graft loss in the first months after kidney transplantation. Lipoxygenase products mediate pro- and anti-inflammatory actions and thus we aimed to correlate the histological reports of renal transplant biopsies with urinary lipoxygenase products concentrations to evaluate their role as a diagnostic marker. This study included a total of 34 kidney transplant recipients: 17 with an acute transplant rejection and 17 controls. LTE4, LTB4, 12-HETE and 15-HETE concentrations were measured by enzyme immunoassay. Urinary lipoxygenase product concentrations were not significantly changed during an acute allograft rejection. Nevertheless, LTB4 concentrations correlated significantly with the body temperature (P ≤ 0.05) 3 months after transplantation, and 12- and 15-HETE concentrations correlated significantly with renal function (P ≤ 0.05) 2 weeks after transplantation. In conclusion, our data show a correlation for LTB4 with the body temperature 3 months after transplantation and urinary 12- and 15-HETE concentrations correlate positively with elevated serum creatinine concentrations but do not predict acute allograft rejection. 相似文献
106.
Ohne ZusammenfassungVortrag, gehalten auf der Tagung der Gesselschaft Deutscher Chemiker, Fachgruppe Lebensmittelchemie, in München am 23. September 1949. 相似文献
107.
ao.Univ.-Prof. DI Dr. Friedrich Schöberl DI Bernhard Zeiringer Mag. Christian Moritz 《?sterreichische Wasser- und Abfallwirtschaft》2014,66(5-6):190-205
The EU Water Framework Directive commits member states to achieve good ecological status in all waterbodies. Artificial or heavily modified waterbodies must reach at least its good ecological potential. In view of these requirements, simple and feasible methods are required in order to evaluate habitat suitability for relevant target species in larger river reaches. Well-developed models for determining the relationship between stream flows and habitat for target species mainly based on micro- and meso-scale already exist. However, the application of such models is complex and time-consuming and consequently limited to relatively short river segments. The objective of this study is to develop a simplified applicable assessment model to evaluate habitat conditions for selected target fish. This model uses hydro-morphological indicators for the habitat assessment and relies on correlative relations between habitat suitability and hydro-morphological features of river stretches (average Froude-number, relative flow width, mean bed slope, relative water depth and flow velocity). The indicators were determined as reach-related averages, derived from 2D model simulations (hydraulic and habitat-specific). Particular emphasis was laid on using a wide range of river stretches with different hydro-morphological characteristics (hydrology, bed substratum, bed structures, degree of braiding, sinuosity of the river course, mean bed width and bed slope). As a result, a set of model equations enables the evaluation of fish habitat conditions in river stretches as a function of flow and morphology. The habitat suitability assessment focuses on four preselected target species: brown trout, European grayling and for low slope rivers common nase and barbel. 相似文献
108.
Yordanka Gluhcheva Irena Pashkunova-Martic Martin Schaier Ivelin Vladov Silviya Stoykova Emilia Petrova Ekaterina Pavlova Peter Dorkov Thomas H. Helbich Bernhard Keppler Juliana Ivanova 《International journal of molecular sciences》2022,23(8)
Lead (Pb) exposure induces severe nephrotoxic effects in humans and animals. Herein, we compare the effects of two chelating agents, salinomycin and deferiprone, on Pb-induced renal alterations in mice and in the homeostasis of essential elements. Adult male mice (Institute of Cancer Research (ICR)) were randomized into four groups: control (Ctrl)—untreated mice administered distilled water for 28 days; Pb-exposed group (Pb)—mice administered orally an average daily dose of 80 mg/kg body weight (BW) lead (II) nitrate (Pb(NO3)2) during the first two weeks of the experimental protocol followed by the administration of distilled water for another two weeks; salinomycin-treated (Pb + Sal) group—Pb-exposed mice, administered an average daily dose of 16 mg/kg BW salinomycin for two weeks; deferiprone-treated (Pb + Def) group—Pb-exposed mice, administered an average daily dose of 20 mg/kg BW deferiprone for 14 days. The exposure of mice to Pb induced significant accumulation of the toxic metal in the kidneys and elicited inflammation with leukocyte infiltrations near the glomerulus. Biochemical analysis of the sera revealed that Pb significantly altered the renal function markers. Pb-induced renal toxicity was accompanied by a significant decrease in the endogenous renal concentrations of phosphorous (P), calcium (Ca), copper (Cu) and selenium (Se). In contrast to deferiprone, salinomycin significantly improved renal morphology in Pb-treated mice and decreased the Pb content by 13.62% compared to the Pb-exposed group. There was also a mild decrease in the renal endogenous concentration of magnesium (Mg) and elevation of the renal concentration of iron (Fe) in the salinomycin-treated group compared to controls. Overall, the results demonstrated that salinomycin is a more effective chelating agent for the treatment of Pb-induced alterations in renal morphology compared to deferiprone. 相似文献
109.
110.
Dipl.-Ing. Dr. mont. Pawel Krajewski Christian Bernhard Roman Krobath Thomas Schaden Sergiu Ilie 《BHM Berg- und Hüttenm?nnische Monatshefte》2014,159(7):304-305
Continuous casting of steel free of surface cracks is still one of the major quality challenges in the whole steel production. The key roles for the phenomenon of surface cracking are played by the critical strain and the temperature-dependent material’s phenomena. The new In-Situ Characterization Bending (IMC-B) method will enable the investigation of the critical strains with respect to the cracking under the main continuous casting boundaries. This publication presents potential and interesting results of the IMC-B experiment. 相似文献