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41.
Summary
A series of new poly(arylene ether 1,3,4-oxadiazole)s has been obtained starting from a difluorosubstituted monomer containing
1,3,4-oxadiazole rings and some dihydroxynaphthalene isomers. The polymers have been prepared by polycondensation in solution
and have been obtained in quantitative yield. They had inherent viscosity from 0.2 to 0.82 dL/g, showed good thermal stability
(10% weight loss temperatures in nitrogen and air were above 460 and 450°C, respectively) and high glass transition temperatures
(in the range of 197–232°C). The polymers were characterized by elemental and infrared analyses, GPC and wide angle X-ray
diffraction.
Received: 27 June 2000/Revised version: 2 October 2000/Accepted: 2 October 2000 相似文献
42.
Anna Di Gianni Giovanna Colucci Aldo Priola Lucia Conzatti Matteo Alessi Paola Stagnaro 《大分子材料与工程》2009,294(10):705-710
The preparation of new rubber based nanocomposites by using properly modified organophilic clays is described. A commercial organophilic montmorillonite containing a hydroxylated ammonium ion is reacted with LPBs. The reaction causes a decrease of the polarity of the clay and a great increase of the interlayer distance. The modified organoclays are successfully dispersed into rubber matrices (SBR or BR) by melt blending in an internal batch mixer. SAXS analyses and TEM micrographs revealed the formation of highly exfoliated nanocomposites containing intercalated stacks made of few lamellae.
43.
Franck Paganelli Giovanna Mottola Julien Fromonot Marion Marlinge Pierre Deharo Rgis Guieu Jean Ruf 《International journal of molecular sciences》2021,22(4)
The influence of hyperhomocysteinemia (HHCy) on cardiovascular disease (CVD) remains unclear. HHCy is associated with inflammation and atherosclerosis, and it is an independent risk factor for CVD, stroke and myocardial infarction. However, homocysteine (HCy)-lowering therapy does not affect the inflammatory state of CVD patients, and it has little influence on cardiovascular risk. The HCy degradation product hydrogen sulfide (H2S) is a cardioprotector. Previous research proposed a positive role of H2S in the cardiovascular system, and we discuss some recent data suggesting that HHCy worsens CVD by increasing the production of H2S, which decreases the expression of adenosine A2A receptors on the surface of immune and cardiovascular cells to cause inflammation and ischemia, respectively. 相似文献
44.
Rodrigo F. Ortiz-Meoz Liping Wang Rosalie Matico Anna Rutkowska-Klute Martha De la Rosa Sabrina Bedard Robert Midgett Katrin Strohmer Douglas Thomson Cunyu Zhang Makda Mebrahtu Jeffrey Guss Rachel Totoritis Thomas Consler Nino Campobasso David Taylor Tia Lewis Kurt Weaver Marcel Muelbaier John Seal Richard Dunham Wieslaw Kazmierski David Favre Giovanna Bergamini Lisa Shewchuk Alan Rendina Guofeng Zhang 《Chembiochem : a European journal of chemical biology》2021,22(3):516-522
Indoleamine-2,3-dioxygenase 1 (IDO1) is a heme-containing enzyme that catalyzes the rate-limiting step in the kynurenine pathway of tryptophan (TRP) metabolism. As it is an inflammation-induced immunoregulatory enzyme, pharmacological inhibition of IDO1 activity is currently being pursued as a potential therapeutic tool for the treatment of cancer and other disease states. As such, a detailed understanding of the mechanism of action of IDO1 inhibitors with various mechanisms of inhibition is of great interest. Comparison of an apo-form-binding IDO1 inhibitor (GSK5628) to the heme-coordinating compound, epacadostat (Incyte), allows us to explore the details of the apo-binding inhibition of IDO1. Herein, we demonstrate that GSK5628 inhibits IDO1 by competing with heme for binding to a heme-free conformation of the enzyme (apo-IDO1), whereas epacadostat coordinates its binding with the iron atom of the IDO1 heme cofactor. Comparison of these two compounds in cellular systems reveals a long-lasting inhibitory effect of GSK5628, previously undescribed for other known IDO1 inhibitors. Detailed characterization of this apo-binding mechanism for IDO1 inhibition might help design superior inhibitors or could confer a unique competitive advantage over other IDO1 inhibitors vis-à-vis specificity and pharmacokinetic parameters. 相似文献
45.
Dr. Vladimir O. Talibov Dr. Edoardo Fabini Edward A. FitzGerald Dr. Daniele Tedesco Daniela Cederfeldt Martin J. Talu Moira M. Rachman Filip Mihalic Dr. Elisabetta Manoni Dr. Marina Naldi Dr. Paola Sanese Dr. Giovanna Forte Dr. Martina Lepore Signorile Prof. Xavier Barril Dr. Cristiano Simone Prof. Manuela Bartolini Dr. Doreen Dobritzsch Dr. Alberto Del Rio Prof. U. Helena Danielson 《Chembiochem : a European journal of chemical biology》2021,22(9):1597-1608
SMYD3 is a multifunctional epigenetic enzyme with lysine methyltransferase activity and various interaction partners. It is implicated in the pathophysiology of cancers but with an unclear mechanism. To discover tool compounds for clarifying its biochemistry and potential as a therapeutic target, a set of drug-like compounds was screened in a biosensor-based competition assay. Diperodon was identified as an allosteric ligand; its R and S enantiomers were isolated, and their affinities to SMYD3 were determined (KD=42 and 84 μM, respectively). Co-crystallization revealed that both enantiomers bind to a previously unidentified allosteric site in the C-terminal protein binding domain, consistent with its weak inhibitory effect. No competition between diperodon and HSP90 (a known SMYD3 interaction partner) was observed although SMYD3–HSP90 binding was confirmed (KD=13 μM). Diperodon clearly represents a novel starting point for the design of tool compounds interacting with a druggable allosteric site, suitable for the exploration of noncatalytic SMYD3 functions and therapeutics with new mechanisms of action. 相似文献
46.
Delfino Chamorro-Arenas Giovanna Salgado-Moreno Dr. Liliana Martinez-Mendieta Dr. Leticia Quintero Dr. Beatriz Godínez-Chaparro Prof. Fernando Sartillo-Piscil 《ChemMedChem》2021,16(3):472-476
The design, stereoselective synthesis and in vivo antiallodynic activity of four novel paroxetine analogs, named 3-hydroxy paroxetines (3HPXs), is reported herein. Among the novel synthesized compounds, three showed an antiallodynic effect, while (R,R)-3HPX was found to be 2.5 times more bioactive than (-)-paroxetine itself in neuropathic rats. Consequently, the current investigation not only discloses a novel promising analgesic drug, but also reveals that functionalization at the C3 position of paroxetine could be as effective as the common functionalization at either C4 or within the sesamol group. 相似文献
47.
Prof. Alessia Carocci Dr. Mariagrazia Roselli Prof. Roberta Budriesi Dr. Matteo Micucci Prof. Jean-François Desaphy Dr. Concetta Altamura Dr. Maria Maddalena Cavalluzzi Dr. Maddalena Toma Dr. Giovanna Ilaria Passeri Dr. Gualtiero Milani Dr. Angelo Lovece Prof. Alessia Catalano Dr. Claudio Bruno Dr. Annalisa De Palma Prof. Filomena Corbo Prof. Carlo Franchini Prof. Solomon Habtemariam Prof. Giovanni Lentini 《ChemMedChem》2021,16(3):578-588
Under the hypothesis that cardioprotective agents might benefit from synergism between antiarrhythmic activity and antioxidant properties, a small series of mexiletine analogues were coupled with the 2,2,5,5-tetramethylpyrroline moiety, known for its antioxidant effect, in order to obtain dual-acting drugs potentially useful in the protection of the heart against post-ischemic reperfusion injury. The pyrroline derivatives reported herein were found to be more potent as antiarrhythmic agents than mexiletine and displayed antioxidant activity. The most interesting tetramethylpyrroline congener, a tert-butyl-substituted analogue, was at least 100 times more active as an antiarrhythmic than mexiletine. 相似文献
48.
Raffaella Balestrini Cecilia Brunetti Maria Cammareri Sofia Caretto Valeria Cavallaro Eleonora Cominelli Monica De Palma Teresa Docimo Giovanna Giovinazzo Silvana Grandillo Franca Locatelli Erica Lumini Dario Paolo Cristina Patan Francesca Sparvoli Marina Tucci Elisa Zampieri 《International journal of molecular sciences》2021,22(6)
Plant specialized metabolites (SMs) play an important role in the interaction with the environment and are part of the plant defense response. These natural products are volatile, semi-volatile and non-volatile compounds produced from common building blocks deriving from primary metabolic pathways and rapidly evolved to allow a better adaptation of plants to environmental cues. Specialized metabolites include terpenes, flavonoids, alkaloids, glucosinolates, tannins, resins, etc. that can be used as phytochemicals, food additives, flavoring agents and pharmaceutical compounds. This review will be focused on Mediterranean crop plants as a source of SMs, with a special attention on the strategies that can be used to modulate their production, including abiotic stresses, interaction with beneficial soil microorganisms and novel genetic approaches. 相似文献
49.
Fatou Ndoye Muhammad Sulaiman Yousafzai Giovanna Coceano Serena Bonin Giacinto Scoles Oumar Ka 《International Journal of Optomechatronics》2016,10(1):53-62
We studied the lateral forces arising during the vertical indentation of the cell membrane by an optically trapped microbead, using back focal plane interferometry to determine force components in all directions. We analyzed the cell-microbead interaction and showed that indeed the force had also lateral components. Using the Hertz model, we calculated and compared the elastic moduli resulting from the total and vertical forces, showing that the differences are important and the total force should be considered. To confirm our results we analyzed cells from two breast cancer cell lines: MDA-MB-231 and HBL-100, known to have different cancer aggressiveness and hence stiffness. 相似文献
50.
Maria Gaetana Giovanna Pittal Stefano Conti Nibali Simona Reina Vincenzo Cunsolo Antonella Di Francesco Vito De Pinto Angela Messina Salvatore Foti Rosaria Saletti 《International journal of molecular sciences》2021,22(23)
VDAC (voltage-dependent anion selective channel) proteins, also known as mitochondrial porins, are the most abundant proteins of the outer mitochondrial membrane (OMM), where they play a vital role in various cellular processes, in the regulation of metabolism, and in survival pathways. There is increasing consensus about their function as a cellular hub, connecting bioenergetics functions to the rest of the cell. The structural characterization of VDACs presents challenging issues due to their very high hydrophobicity, low solubility, the difficulty to separate them from other mitochondrial proteins of similar hydrophobicity and the practical impossibility to isolate each single isoform. Consequently, it is necessary to analyze them as components of a relatively complex mixture. Due to the experimental difficulties in their structural characterization, post-translational modifications (PTMs) of VDAC proteins represent a little explored field. Only in recent years, the increasing number of tools aimed at identifying and quantifying PTMs has allowed to increase our knowledge in this field and in the mechanisms that regulate functions and interactions of mitochondrial porins. In particular, the development of nano-reversed phase ultra-high performance liquid chromatography (nanoRP-UHPLC) and ultra-sensitive high-resolution mass spectrometry (HRMS) methods has played a key role in this field. The findings obtained on VDAC PTMs using such methodologies, which permitted an in-depth characterization of these very hydrophobic trans-membrane pore proteins, are summarized in this review. 相似文献