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61.
Bu HZ Magis L Knuth K Teitelbaum P 《Rapid communications in mass spectrometry : RCM》2001,15(10):741-748
The inhibition potential of drugs towards five major human hepatic cytochrome P450 (CYP) isozymes (CYP2A6, 3A4, 2C9, 2D6, and 2E1) was investigated via cassette dosing of the five probe substrates (coumarin, midazolam, tolbutamide, dextromethorphan, and chlorzoxazone) in human liver microsomes using a 96-well plate format. After microsomal incubations had been terminated with formic acid, the five marker metabolites (7-hydroxycoumarin, 1'-hydroxymidazolam, 4-hydroxytolbutamide, dextrorphan, and 6-hydroxychlorzoxazone) were simultaneously quantified using direct injection/online guard cartridge extraction/tandem mass spectrometry (DI-GCE/MS/MS). Several advantages resulted from the use of a short C(18) guard cartridge (4 mm in length) for DI-GCE/MS/MS, including minimal sample preparation, fast online extraction, short analysis time (2.5 min), and minimal source contamination. In addition, this method demonstrated an inter-day accuracy range from -8.7 - 7.4% with a precision less than 8.3% for the quantification of all the marker metabolites. The inhibition assay for the five CYP isozymes was evaluated using their known selective inhibitors via individual and cassette dosing of the probe substrates. The IC(50) values measured via cassette dosing were consistent with those observed via individual dosing, which were all in agreement with the reported values. In addition, the validated assay was used to evaluate the inhibitory potential of 23 generic drugs (randomly selected) towards the five CYP isozymes. The results suggest the integration of the cassette dosing strategy and the DI-GCE/MS/MS method can provide a reliable in vitro approach to screening the inhibitory potential of new chemical entities, with maximal throughput and cost-effectiveness, in support of drug discovery and development. 相似文献
62.
Yu-Dong Shen Hai-Qiang Wu Xian-Zhang Bu Lin-Kun An Pei-Qing Liu Yue-Ming Li 《Tetrahedron》2005,61(38):9097-9101
A novel procedure to construct o-naphthothiophenequinones has been achieved from readily available o-benzothiophenquinones and N-dienes via Diels-Alder reaction-aromatization sequence as key steps. The absolute regioselectivity was established via Diels-Alder reaction of o-benzothiophenquinones with rich electron N-dienes. 相似文献
63.
Long Bu 《Microelectronics Journal》2006,37(8):828-836
This paper demonstrates a keyword match processor capable of performing fast dictionary search with approximate match capability. Using a content addressable memory with processor element cells, the processor can process arbitrary sized keywords and match input text streams in a single clock cycle. We present an architecture that allows priority detection of multiple keyword matches on single input strings. The processor is capable of determining approximate match and providing distance information as well. A 64-word design has been developed using 19,000 transistors and it could be expanded to larger sizes easily. Using a modest 0.5 μm process, we are achieving cycle times of 10 ns and the design will scale to smaller feature sizes. 相似文献
64.
文献[1]提出的最优加权空间平滑技术可以使相干源存在时的信源协方差矩阵恢复为对角阵.由于文献[1]中导出的最优权矩阵是空间信源方位的函数矩阵,本文利用最优加权空间平滑后阵列协方差矩阵的Toeplitz性,构造了一个全新的优化拟合的代价函数,并基于此提出了一种相干源方位估计的新算法.与文献[1]不同,算法的实现不需要方位估计的先验知识和协方差矩阵的去噪预处理.分辨性能的蒙特卡罗仿真实验表明,新算法对空间相干信源的分辨性能优于常规的空间平滑算法和最大似然算法,在小阵列和信源空间间隔较近时,算法的优越性尤为突出. 相似文献
65.
Dandan Bu Yuying Wang Na Wu Wei Feng Donghui Wei Zhanxian Li Mingming Yu 《中国化学快报》2021,32(5):1799-1802
Based on 4-bromo-1,8-naphthalic anhydride, one novel ratiometric fluorescence H2S-probe (IDNA) was designed and synthesized. Further studies indicate that IDNA can sensitively recognize H2S (detection limit of 7 μmol/L) with good selectivity and anti-interference ability. In addition, IDNA has satisfactory photostability in HeLa cells, ability of mitochondrial co-localization, and can be utilized in fluorescence imaging of H2S. 相似文献
66.
正Molecular materials,together with metals,ceramics,and polymer materials,are among the most important materials.The research efforts on molecular materials are targeting three main aspects,namely the assembly technique,multi-functionality,and their diverse application.In this regard,the main attention from the community is focused on the identification and 相似文献
67.
Meng-Yue Guo Gen Li Shuai-Liang Yang Ran Bu Xian-Qing Piao Prof. En-Qing Gao 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(66):16415-16421
The assembly of two tripyridinium-tricarboxylate ligands and different metal ions leads to seven isostructural MOFs, which show novel 2D→2D supramolecular entanglement featuring catenane-like interlocking of tricyclic cages. The MOFs show tripyridinium-afforded and metal-modulated photoresponsive properties. The MOFs with d10 metal centers ( 1-Cd , 1-Zn , 2-Cd , 2-Zn ) show fast and reversible photochromism and concomitant fluorescence quenching, 1-Ni displays slower photochromism but does not fluoresce, and 1-Co and 2-Co are neither photochromic nor fluorescent. It is shown here that the network entanglement dictates donor-acceptor close contacts, which enable fluorescence originated from interligand charge transfer. The contacts also allow photoinduced electron transfer, which underlies photochromism and concomitant fluorescence response. The metal dependence in fluorescence and photochromism can be related to energy transfer through metal-centered d-d transitions. In addition, 1-Cd is demonstrated to be a potential fluorescence sensor for sensitive and selective detection of UO22+ in water. 相似文献
68.
Shuyang Liu Miao Tian Dr. Xiubin Bu Dr. Hua Tian Prof. Xiaobo Yang 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(28):7738-7744
Photoactive two-dimensional covalent organic frameworks (2D-COFs) have become promising heterogenous photocatalysts in visible-light-driven organic transformations. Herein, a visible-light-driven selective aerobic oxidation of various small organic molecules by using 2D-COFs as the photocatalyst was developed. In this protocol, due to the remarkable photocatalytic capability of hydrazone-based 2D-COF-1 on molecular oxygen activation, a wide range of amides, quinolones, heterocyclic compounds, and sulfoxides were obtained with high efficiency and excellent functional group tolerance under very mild reaction conditions. Furthermore, benefiting from the inherent advantage of heterogenous photocatalysis, prominent sustainability and easy photocatalyst recyclability, a drug molecule (modafinil) and an oxidized mustard gas simulant (2-chloroethyl ethyl sulfoxide) were selectively and easily obtained in scale-up reactions. Mechanistic investigations were conducted using radical quenching experiments and in situ ESR spectroscopy, all corroborating the proposed role of 2D-COF-1 in photocatalytic cycle. 相似文献
69.
70.
We study the well‐posedness of the fractional differential equations with infinite delay on Lebesgue–Bochner spaces and Besov spaces , where A and B are closed linear operators on a Banach space X satisfying , and . Under suitable assumptions on the kernels a and b, we completely characterize the well‐posedness of in the above vector‐valued function spaces on by using known operator‐valued Fourier multiplier theorems. We also give concrete examples where our abstract results may be applied. 相似文献