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101.
Matthew J. Bauer Catherine S. Snyder Christopher C. Bowland Amanda M. Uhl Maeve A. K. Budi Maria Villancio‐Wolter Henry A. Sodano Jennifer S. Andrew 《Journal of the American Ceramic Society》2016,99(12):3902-3908
Barium titanate nanofibers were uniaxially aligned by electrospinning onto a rotating copper wire drum and alignment was maintained during calcination of the fibers. Two methods for maintaining alignment during calcination were tested, by either using carbon tape or a peeling off method to remove the aligned fibers from the mandrel followed by calcination. The carbon tape removal method led to the formation of shorter aligned nanowires while the peeling off method resulted in longer nanofibers. Additionally, the effects of calcination temperature and time on crystal structure were also examined. The degree of tetragonality in the barium titanate nanofibers increased at higher calcination temperatures and times. Piezoelectricity was confirmed in the nanofibers calcined using piezoeresponse force microscopy, yielding a d33 value of 15.5 pm/V. Using the methods presented here, large quantities of aligned piezoelectric barium titanate and other ceramic fibers or wires can be produced to fulfill their demand in novel microelectronics. 相似文献
102.
Poly(butylene succinate‐co‐butylene adipate)/polyethylene oxide blends for controlled release materials: A morphological study
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Amandine Cottaz Fadi Khalil Sophie Galland Fouzia Jbilou Isabelle Adt Pascal Degraeve Catherine Joly 《应用聚合物科学杂志》2016,133(3)
Varying the formulation and processing conditions of polymer blends allows the design of materials with a large range of morphologies. Active materials embedding active compounds in a devoted phase are promising applications of such blends, offering possible various transport properties. In this study, 13 poly(butylene succinate‐co‐butylene adipate) (PBSA)/polyethylene oxide (PEO) blends were extruded in a slit die. Their morphologies were characterized by water extraction (selective PEO dissolution), FTIR spectroscopy, and differential scanning calorimetry. Transport properties were assessed by water vapor permeation and fluorescein release as model migrant. Indeed, the desorption in water of fluorescein (previously entrapped in PEO) was monitored to preliminary investigate the release properties of these materials: two morphologies were obtained (i) pseudo multilayer films made of PEO‐rich layer/PBSA‐rich layer/PEO‐rich layer and (ii) PEO nodules dispersed in the PBSA‐rich matrix for the highest PBSA contents. The first systems were erodible ones with an uncontrolled fast delivery by PEO dissolution whereas the second ones showed a controlled release by permeation through the PBSA matrix from PEO nodules. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 42874. 相似文献
103.
Activity of Fluorine‐Containing Analogues of WC‐9 and Structurally Related Analogues against Two Intracellular Parasites: Trypanosoma cruzi and Toxoplasma gondii
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María N. Chao Catherine Li Melissa Storey Dr. Bruno N. Falcone Dr. Sergio H. Szajnman Prof. Dr. Sergio M. Bonesi Prof. Dr. Roberto Docampo Prof. Dr. Silvia N. J. Moreno Prof. Dr. Juan B. Rodriguez 《ChemMedChem》2016,11(24):2690-2702
Two obligate intracellular parasites, Trypanosoma cruzi, the agent of Chagas disease, and Toxoplasma gondii, an agent of toxoplasmosis, upregulate the mevalonate pathway of their host cells upon infection, which suggests that this host pathway could be a potential drug target. In this work, a number of compounds structurally related to WC‐9 (4‐phenoxyphenoxyethyl thiocyanate), a known squalene synthase inhibitor, were designed, synthesized, and evaluated for their effect on T. cruzi and T. gondii growth in tissue culture cells. Two fluorine‐containing derivatives, the 3‐(3‐fluorophenoxy)‐ and 3‐(4‐fluorophenoxy)phenoxyethyl thiocyanates, exhibited half‐maximal effective concentration (EC50) values of 1.6 and 4.9 μm , respectively, against tachyzoites of T. gondii, whereas they showed similar potency to WC‐9 against intracellular T. cruzi (EC50 values of 5.4 and 5.7 μm , respectively). In addition, 2‐[3‐ (phenoxy)phenoxyethylthio]ethyl‐1,1‐bisphosphonate, which is a hybrid inhibitor containing 3‐phenoxyphenoxy and bisphosphonate groups, has activity against T. gondii proliferation at sub‐micromolar levels (EC50=0.7 μm ), which suggests a combined inhibitory effect of the two functional groups. 相似文献
104.
Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold‐Hopping Approach
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Dr. Bibia Heidmann Dr. John Gatfield Dr. Catherine Roch Dr. Alexander Treiber Dr. Simone Tortoioli Dr. Christine Brotschi Dr. Jodi T. Williams Dr. Martin H. Bolli Dr. Stefan Abele Dr. Thierry Sifferlen Dr. François Jenck Dr. Christoph Boss 《ChemMedChem》2016,11(19):2132-2146
Starting from suvorexant (trade name Belsomra), we successfully identified interesting templates leading to potent dual orexin receptor antagonists (DORAs) via a scaffold‐hopping approach. Structure–activity relationship optimization allowed us not only to improve the antagonistic potency on both orexin 1 and orexin 2 receptors (Ox1 and Ox2, respectively), but also to increase metabolic stability in human liver microsomes (HLM), decrease time‐dependent inhibition of cytochrome P450 (CYP) 3A4, and decrease P‐glycoprotein (Pgp)‐mediated efflux. Compound 80 c [{(1S,6R)‐3‐(6,7‐difluoroquinoxalin‐2‐yl)‐3,8‐diazabicyclo[4.2.0]octan‐8‐yl}(4‐methyl‐[1,1′‐biphenyl]‐2‐yl)methanone] is a potent and selective DORA that inhibits the stimulating effects of orexin peptides OXA and OXB at both Ox1 and Ox2. In calcium‐release assays, 80 c was found to exhibit an insurmountable antagonistic profile at both Ox1 and Ox2, while displaying a sleep‐promoting effect in rat and dog models, similar to that of the benchmark compound suvorexant. 相似文献
105.
Mallory Batty Rachel Pugh Ilampirai Rathinam Joshua Simmonds Edwin Walker Amanda Forbes Shailendra Anoopkumar-Dukie Catherine M. McDermott Briohny Spencer David Christie Russ Chess-Williams 《International journal of molecular sciences》2016,17(8)
This review evaluates the role of α-adrenoceptor antagonists as a potential treatment of prostate cancer (PCa). Cochrane, Google Scholar and Pubmed were accessed to retrieve sixty-two articles for analysis. In vitro studies demonstrate that doxazosin, prazosin and terazosin (quinazoline α-antagonists) induce apoptosis, decrease cell growth, and proliferation in PC-3, LNCaP and DU-145 cell lines. Similarly, the piperazine based naftopidil induced cell cycle arrest and death in LNCaP-E9 cell lines. In contrast, sulphonamide based tamsulosin did not exhibit these effects. In vivo data was consistent with in vitro findings as the quinazoline based α-antagonists prevented angiogenesis and decreased tumour mass in mice models of PCa. Mechanistically the cytotoxic and antitumor effects of the α-antagonists appear largely independent of α 1-blockade. The proposed targets include: VEGF, EGFR, HER2/Neu, caspase 8/3, topoisomerase 1 and other mitochondrial apoptotic inducing factors. These cytotoxic effects could not be evaluated in human studies as prospective trial data is lacking. However, retrospective studies show a decreased incidence of PCa in males exposed to α-antagonists. As human data evaluating the use of α-antagonists as treatments are lacking; well designed, prospective clinical trials are needed to conclusively demonstrate the anticancer properties of quinazoline based α-antagonists in PCa and other cancers. 相似文献
106.
Venkat N. Vangaveti Venkatesh M. Shashidhar Catherine Rush Usman H. Malabu Roy R. Rasalam Fiona Collier Bernhard T. Baune Richard L. Kennedy 《Lipids》2014,49(12):1181-1192
Macrophage apoptosis, a key process in atherogenesis, is regulated by oxidation products, including hydroxyoctadecadienoic acids (HODEs). These stable oxidation products of linoleic acid (LA) are abundant in atherosclerotic plaque and activate PPARγ and GPR132. We investigated the mechanisms through which HODEs regulate apoptosis. The effect of HODEs on THP‐1 monocytes and adherent THP‐1 cells were compared with other C18 fatty acids, LA and α‐linolenic acid (ALA). The number of cells was reduced within 24 hours following treatment with 9‐HODE (p < 0.01, 30 μM) and 13 HODE (p < 0.01, 30 μM), and the equivalent cell viability was also decreased (p < 0.001). Both 9‐HODE and 13‐HODE (but not LA or ALA) markedly increased caspase‐3/7 activity (p < 0.001) in both monocytes and adherent THP‐1 cells, with 9‐HODE the more potent. In addition, 9‐HODE and 13‐HODE both increased Annexin‐V labelling of cells (p < 0.001). There was no effect of LA, ALA, or the PPARγ agonist rosiglitazone (1μM), but the effect of HODEs was replicated with apoptosis‐inducer camptothecin (10μM). Only 9‐HODE increased DNA fragmentation. The pro‐apoptotic effect of HODEs was blocked by the caspase inhibitor DEVD‐CHO. The PPARγ antagonist T0070907 further increased apoptosis, suggestive of the PPARγ‐regulated apoptotic effects induced by 9‐HODE. The use of siRNA for GPR132 showed no evidence that the effect of HODEs was mediated through this receptor. 9‐HODE and 13‐HODE are potent—and specific—regulators of apoptosis in THP‐1 cells. Their action is PPARγ‐dependent and independent of GPR132. Further studies to identify the signalling pathways through which HODEs increase apoptosis in macrophages may reveal novel therapeutic targets for atherosclerosis. 相似文献
107.
Poly(Tetrasubstituted Aryl Imidazole)s (PTAIs), a new class of poly(heteroaromatic) polymers was prepared via a cascade polycondensation process, under microwave irradiation. These polymers were obtained by the tetrasubstituted aryl imidazole ring formation involving bis(aryl α-diketone)s, bis(arylaldehyde)s, mono(arylamine)s and ammonium acetate. The polymerization performed under microwave irradiation allowed to get high molecular weight PTAIs in very short reaction times. The chemical structure of these PTAIs was confirmed by NMR spectroscopy. Thermogravimetric analyses (TGA) showed a very good grade of thermal stability of these polymers. Glass transition temperatures (Tg) of PTAIs ranging from 155 °C to 265 °C were determined by Differential Scanning Calorimetry (DSC). 相似文献
108.
Ian Mabbett Jon Elvins Catherine Gowenlock Carol Glover Paul Jones Geraint Williams David Worsley 《Progress in Organic Coatings》2014
Near infrared (NIR) is becoming a popular option for rapid cure of coatings in the coil coating industry particularly where fast line speeds are required. The technology has the potential to reduce the cure time of a 20 μm polyester coating on a galvanised steel substrate from around 30 s via conventional heating methods down to <10 s under the lamps. Previous work suggested that the ideal situation in this case is to have a topcoat which is slightly transparent to NIR and an absorbing substrate to heat the coating from the substrate outwards in a two stage process which separates solvent removal from cross linking and film formation. This can be taken further by tinting the primer layer with a pigment that absorbs in the NIR region. In this study spectroscopy was used to show that a coated steel system could appear white in the visible region because of the reflectance of TiO2 but the NIR absorption could be altered by adding absorbing pigments such as carbon black. Lamp settings could be reduced by 20% to achieve equivalent cure with tinted primer systems. The potential degradation in corrosion protection afforded by carbon-black containing pigments at various loadings was assessed for model organic coatings applied to galvanised steel specimens. In situ scanning Kelvin probe studies showed that rates of corrosion-driven coating delamination by cathodic disbondment remained unchanged by pigment loadings of up to 3.5 wt%. 相似文献
109.
110.