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41.
Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9‐Epipolygodial against Drug‐Resistant Cancer Cells 下载免费PDF全文
Dr. Ramesh Dasari Annelise De Carvalho Derek C. Medellin Kelsey N. Middleton Dr. Frédéric Hague Marie N. M. Volmar Prof. Liliya V. Frolova Dr. Mateus F. Rossato Jorge J. De La Chapa Nicholas F. Dybdal‐Hargreaves Akshita Pillai Prof. Véronique Mathieu Prof. Snezna Rogelj Prof. Cara B. Gonzales Prof. João B. Calixto Prof. Antonio Evidente Dr. Mathieu Gautier Dr. Gnanasekar Munirathinam Prof. Rainer Glass Prof. Patricia Burth Dr. Stephen C. Pelly Prof. Willem A. L. van Otterlo Prof. Robert Kiss Prof. Alexander Kornienko 《ChemMedChem》2015,10(12):2014-2026
Polygodial, a terpenoid dialdehyde isolated from Polygonum hydropiper L., is a known agonist of the transient receptor potential vanilloid 1 (TRPV1). In this investigation a series of polygodial analogues were prepared and investigated for TRPV1‐agonist and anticancer activities. These experiments led to the identification of 9‐epipolygodial, which has antiproliferative potency significantly exceeding that of polygodial. 9‐Epipolygodial was found to maintain potency against apoptosis‐resistant cancer cells as well as those displaying the multidrug‐resistant (MDR) phenotype. In addition, the chemical feasibility for the previously proposed mechanism of action of polygodial, involving the formation of a Paal–Knorr pyrrole with a lysine residue on the target protein, was demonstrated by the synthesis of a stable polygodial pyrrole derivative. These studies reveal rich chemical and biological properties associated with polygodial and its direct derivatives. These compounds should inspire further work in this area aimed at the development of new pharmacological agents, or the exploration of novel mechanisms of covalent modification of biological molecules with natural products. 相似文献
42.
The urban-rural planning inspector system of China is hierarchical supervision over local governments from the Central Government in respect of town and country development. The comparative analysis on planning inspection system of the UK may provide experience in seeking solutions to the problems occurring in the system of China. The planning inspector system of China can be improved in six aspects such as establishing the legal status, setting up the planning inspection agency, completing the personnel management system, enhancing the legal binding force, building the internal and external supervision channel, supplementing the relieve function, and establishing the coordination mechanism of various internal supervisions. 相似文献
43.
P. JideshAuthor Vitae Santhosh George Author Vitae 《Computers & Electrical Engineering》2012,38(5):1262-1277
In this paper a shock coupled fourth-order diffusion filter is proposed for image enhancement. This filter converges at a faster rate while preserving and enhancing edges, ramps and textures present in the images. The proposed filter diffuses with varying magnitudes in the directions normal to the level-curve and along it. The magnitude of the directional diffusion is controlled by a diffusion function, meant to provide a good response in the direction along the level-curves, than across them. The proposed filter can still preserve the planar approximation of the image, thereby avoiding the discrepancy caused due to the staircase effect, as in the second-order counterparts. The anisotropic property of the filter is thoroughly studied, analyzed and demonstrated with perspective and quantitative results. The performance of the proposed filter is compared with the state-of-the-art methods for image enhancement. The quantitative and perspective measures provided endorse the capability of the method to enhance various kinds of images. 相似文献
44.
Characterizing cerebral oxygen metabolism employing oxygen-17 MRI/MRS at high fields 总被引:1,自引:1,他引:0
Ali Gordji-Nejad Klaus Möllenhoff Ana Maria Oros-Peusquens Deepu R. Pillai Nadim Jon Shah 《Magma (New York, N.Y.)》2014,27(1):81-93
This article provides a comprehensive overview of oxygen (17O) magnetic resonance spectroscopy and imaging, including the advantages and challenges offered by the different methods developed thus far. The physiological role and relevance of oxygen, and its participation in aerobic metabolism, are addressed to emphasize the importance of the investigations and the efforts related to these developments. Furthermore, a number of methods employed in the determination of the cerebral metabolic rate of oxygen in neural cells will be presented, focusing primarily on methodologies enabling absolute quantification. 相似文献
45.
Mabel Ebenezer Rajkumar Mattacaud Ramachandralal Chandramohanan Nair Padmanabha Pillai Sarasamma 《电力部件与系统》2015,43(20):2251-2261
Transformers are critical components in power systems and their failure can cause long interruption of power supply. The condition of a transformer can be monitored by performing thermal analysis. The use of non-linear devices, such as rectifiers and converters, draws harmonic currents that increase losses in transformers, thereby increasing their operating temperature. In this article, a new numerical approach is presented for determining the rise in hot spot temperature in a 5-kVA, 400/400-V dry-type three-phase transformer laboratory prototype. The key novelty is that the additional winding eddy current loss due to non-linear loads is considered in the numerical modeling. The winding eddy current loss corresponding to harmonic distortion is estimated by conducting experiments and calculations. Numerical simulations are carried out for a wide range of non-linear loads using a commercial computational fluid dynamics package, FLUENT 6.3. The proposed numerical methodology is validated by performing experiments on the transformer for possible non-linear loads and comparing the measured hot spot temperature with the simulated values. Correlation equations for rise in hot spot temperature as a function of total harmonic distortion are presented, which can be used for estimating the life of transformers when connected to different types of loads. 相似文献
46.
Sangita Kumari Karthikeyan Pillai Asha Sharma Ella Mihevc Amit Srivastava Albert Chan 《Particulate Science and Technology》2015,33(5):562-566
Cryogenic aerosol cleaning is a dry cleaning method used in the back end of line (BEOL) semiconductor manufacturing to remove defects from planar hydrophobic surfaces such as SiCOH and SiCxNyHz. Cryogenic aerosol cleaning is preferred over conventional wet cleaning methods as it is a non-contact cleaning method, which uses inert gases to generate sub-micrometer-sized solid aerosol particles that physically remove nanometer-sized contaminants on wafer surfaces. Particle removal mechanism involves detachment of the particles upon impact with aerosol, diffusion, and finally entrainment away from the wafer. In BEOL metal line patterning, particles on the dielectric isolation surfaces translate through the subsequent lithography and copper fill steps in to single or multiple metal line open defects that are yield killers. In this study, we show that the particle removal performance of the standard aerosol cleaning can be enhanced by pre-heating the wafer and use of a higher molecular weight inert gas, namely Ar, for aerosol generation. Both the addition of a Pre-heat step and the use of Ar as the aerosol source showed 47–52% reduction in single and multiple line opens detected through wafer electrical tests during high volume semiconductor manufacturing process. 相似文献
47.
The thermal performance of a passive solar house in Ireland having high energy conservation standards is compared with that of a similar sized conventional dwelling house. In both cases the performance over a meteorological Test Reference Year is assessed using climatically responsive models developed experimentally which predict their internal temperature without heating. The results indicate that the conventional house required over three times as much auxiliary heating as the passive solar house. Solar gain accounted for over half the gross heat demand in the solar house compared to 13% in the bungalow. An added advantage of the increased utilization of solar gain was the estimated reduction in the heating season from nine to six months. 相似文献
48.
Substantial controversy has been produced from the location of over 4000 wind turbines in San Gorgonio Pass, California. The principal point of controversy is the conflicting land use which results from developing wind power in a populated area. A public opinion survey was conducted which demonstrated that the vocal opposition to the wind turbines so commonly expressed is not borne out in fact. While there is indeed some opposition to the development of wind power at this site, particularly in terms of aesthetic degradation, the majority of respondents favoured the development. This level of approval will be of interest to those developing large wind projects elsewhere. 相似文献
49.
Solar stills have been designed to produce water for use in teaching and research laboratories. Various designs and configurations have been constructed and tested over the past 10 years. The original double-surfaced cascade stills (stills A and B) were constructed in aluminium and were rather expensive. Later models termed Series D and E were of galvanised mild steel with stainless steel distillate drains and safety overflow drains. These galvanised steel units suffered from severe corrosion after a few years of operation. The latest design series F, is built in aluminium with stainless steel distillate drains and automatic feed valves. All of the stills produce very pure distilled water (conductance ~1.5 × 10?6 Ω?1 cm?1; pH 6.8–7.4) at a cost which is below that of conventional electrically heated stills. 相似文献
50.