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61.
62.
Gianluca Ottolina Francesca Gianinetti Sergio Riva Giacomo Carrea 《Catalysis Today》1994,22(3):511-516
The kinetic parameters (Km and Vmax) of lipoprotein lipase (LPL)-catalyzed transesterification were determined in (R)- and (S)-carvone, and in mixtures of the two. It was found that only Vmax was significantly affected by solvent chirality. LPL thermostability was not influenced by solvent config- uration, whereas activation energy was twice as high in (R)-carvone as in (S)-carvone. 相似文献
63.
F Serafini G Vescovo L Dalla Libera C Catani L Facchin PL Tenderini R Zennaro C Leprotti GB Ambrosio 《Canadian Metallurgical Quarterly》1997,42(9):941-946
Chronic heart failure (CHF) is accompanied by a reduced exercise capacity, and the symptoms can be at least in part explained by qualitative and quantitative changes in the skeletal muscle composition and metabolism. We have correlated the myosin heavy chain (MHC) composition of the gastrocnemius in 20 patients with different degrees of CHF to expiratory gases measured during maximal cardiopulmonary exercise testing, NYHA functional class and echocardiographic parameters. MHC composition was determined electrophoretically in skeletal muscle needle microbiopsies and the percent distribution calculated by laser densitometry. There was no correlation between ejection fraction, left ventricular end-diastolic and end-systolic diameters and MHC composition. The percentage of MHC 1 (slow aerobic isoform) was positively correlated with peak VO2 (r2 = 0.5, p = 0.0004), ventilatory threshold (VT, r2 = 0.33, p = 0.008), and O2 pulse (peak VO2/HR, r2 = 0.40, p = 0.003). There was a negative correlation between MHC 2a and 2b (fast isoforms) and peak VO2 (r2 = 0.38 and 0.37, p = 0.004, respectively), VT (r2 = 0.2, p = 0.05; r2 = 0.34, p = 0.007, respectively) and O2 pulse (r2 = 0.39, p = 0.003; r2 = 0.23, p = 0.03, respectively). NYHA functional class was also negatively correlated with the same parameters (r2 = 0.2, p = 0.01; r2 = 0.4, p = 0.001; r2 = 0.34, p = 0.006, respectively) as well as with MHC 1 (r2 = 0.62, p = 0.0001). A positive correlation was found between NYHA functional class and MHC 2a and 2b (r2 = 0.46, p = 0.001; r2 = 0.41, p = 0.002, respectively). The severity of heart failure is paralleled by a shift of the MHC pattern toward the fast MHC 2b. The correlation between the magnitude of the MHCs shift, from the slow aerobic to the fast type, with both clinical parameters (NYHA functional class) and functional measurements (peak VO2, VT, O2 pulse) of exercise capacity seem to suggest that changes in skeletal muscle composition may play a key role in exercise tolerance in patients with CHF. 相似文献
64.
Toward the Development of Dual‐Targeted Glyceraldehyde‐3‐phosphate Dehydrogenase/Trypanothione Reductase Inhibitors against Trypanosoma brucei and Trypanosoma cruzi
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Prof. Dr. Federica Belluti Elisa Uliassi Giacomo Veronesi Dr. Christian Bergamini Dr. Marcel Kaiser Prof. Dr. Reto Brun Angelo Viola Prof. Dr. Romana Fato Prof. Dr. Paul A. M. Michels Prof. Dr. R. Luise Krauth‐Siegel Prof. Dr. Andrea Cavalli Prof. Dr. Maria Laura Bolognesi 《ChemMedChem》2014,9(2):371-382
A significant improvement in the treatment of trypanosomiases has been achieved with the recent development of nifurtimox–eflornithine combination therapy (NECT). As an alternative to drug combinations and as a means to overcome most of the antitrypanosomatid drug discovery challenges, a multitarget drug design strategy has been envisaged. To begin testing this hypothesis, we designed and developed a series of quinone–coumarin hybrids against glyceraldehyde‐3‐phosphate dehydrogenase/trypanothione reductase (GAPDH/TR). These enzymes belong to metabolic pathways that are vital to Trypanosoma brucei and Trypanosoma cruzi, and have thus been considered promising drug targets. The synthesized molecules were characterized for their dual‐target antitrypanosomal profile, both in enzyme assays and in in vitro parasite cultures. The merged derivative 2‐{[3‐(3‐dimethylaminopropoxy)‐2‐oxo‐2H‐chromen‐7‐yl]oxy}anthracene‐1,4‐dione ( 10 ) showed an IC50 value of 5.4 μM against TbGAPDH and a concomitant Ki value of 2.32 μM against TcTR. Notably, 2‐{4‐[6‐(2‐dimethylaminoethoxy)‐2‐oxo‐2H‐chromen‐3‐yl]phenoxy}anthracene‐1,4‐dione (compound 6 ) displayed a remarkable EC50 value for T. brucei parasites (0.026 μM ) combined with a very low cytotoxicity toward mammalian L6 cells (7.95 μM ). This promising low toxicity of compound 6 might be at least partially due to the fact that it does not interfere with human glutathione reductase. 相似文献
65.
66.
The canonical problem of the radiation of an elementary dipole close to a stratified sphere representing a simplified model of human head is investigated in this paper. The proposed approach is a flexible method of investigation about the influence on Specific Absorption Rate (S.A.R.) evaluation of tissue dielectric parameters and geometry as well as a useful tool to test numerical codes. The solution of the electromagnetic (e.m.) problem is achieved in a closed form; results highlight the position of maximum S.A.R. values and their dependence on frequency: for particular layer thicknesses and dielectric parameters, the maximum absorption can occur in the frequency range of cellular phones. 相似文献
67.
G Martinez ML Carnazza C Di Giacomo V Sorrenti M Avitabile A Vanella 《Canadian Metallurgical Quarterly》1998,16(6):519-526
Mutation of the TP53 gene is one of the most common molecular alterations in a variety of tumors, but it occurs infrequently in childhood and adult hematological malignancies. Protein accumulation often results from mutations that lead to inactivation of the p53 protein. Other causes of functional inactivation of the p53 protein include stabilization of p53 via proteins such as MDM2, an oncoprotein capable of forming specific complexes with p53. In the present study, protein expressions of MDM2 and p53 were investigated by immunohistochemistry from bone marrow samples in 23 patients with acute lymphoblastic leukemia aged 1-13 years at diagnosis. p53 protein overexpression was detected in only one case, while overexpression of MDM2 was detected in samples from five patients. All five patients overexpressing MDM2 belonged to a group with unfavorable prognostic signs at diagnosis and three of them relapsed or died within 6 months after diagnosis. 相似文献
68.
Ermanno Barni Piero Savarino Gaetano di Modica Rosarina Carpignano Sisto Sergio Papa Giacomo Giraudo 《Dyes and Pigments》1984,5(1):15-36
Data on a series of 65 azo dyes derived from 4-alkylamido-2-hydroxybenzoic acids are reported. The dyes are suitable for application to polyamide fibres.Many correlations between the nature of substituents and the physical, spectroscopic or tinctorial properties of dyes were established. Correlations between structure and colour of dyed fabrics were also found. 相似文献
69.
G Vescovo L Dalla Libera F Serafini C Leprotti L Facchin M Volterrani C Ceconi GB Ambrosio 《Canadian Metallurgical Quarterly》1998,98(17):1742-1749
BACKGROUND: In congestive heart failure, fatigue-resistant, oxidative, slow type I fibers are decreased in leg skeletal muscle, contributing to exercise capacity (EC) limitation. The mechanisms by which ACE inhibitors and AII antagonists improve EC is still unclear. We tested the hypothesis that improvement in EC is related to changes in skeletal muscle composition toward type I fibers. METHODS AND RESULTS: Eight patients with congestive heart failure, NYHA classes I through IV, were treated for 6 months with enalapril (E) 20 mg/d, and another 8 with losartan (L) 50 mg/d. EC was assessed with maximal cardiopulmonary exercise testing at baseline and after treatment. Myosin heavy chain (MHC) composition of the gastrocnemius was studied after electrophoretic separation of slow MHC1, fast oxidative MHC2a, and fast glycolytic MHC2b isoforms from needle microbiopsies obtained at baseline and after 6 months. EC improved in both groups. Peak V(O2) increased from 21.0+/-4.7 to 27.6+/-4.3 mL . kg-1 . min -1 (P=0.011) in the L group and from 17.5+/-5.0 to 25.0+/-5.5 mL . kg-1 . min -1 (P=0.014) in the E group. Similarly, ventilatory threshold changed from 15.0+/-4.0 to 19.9+/-4.9 mL (P=0. 049) with L and from 12.0+/-1.9 to 15.4+/-3.5 mL (P=0.039) with E. MCH1 increased from 61.2+/-11.2% to 75.4+/-7.6% with L (P=0.012) and from 60.6+/-13.1% to 80.1+/-10.9% (P=0.006) with E. Similarly, MHC2a decreased from 21.20+/-9.5% to 12.9+/-4.4% (P=0.05) with L and from 19.9+/-7.8% to 11.8+/-7.9% (P=0.06) with E. MHC2b changed from 17. 5+/-6.5% to 11.7+/-5.2% (P=0.07) with L and from 19.5+/-6.4% to 8. 1+/-4.6% (P=0.0015) with E. There was a significant correlation between net changes in MHC1 and absolute changes in peak V(O2) (r2=0.29, P=0.029) and a trend to significance for MHC2a and 2b. CONCLUSIONS: Six months' treatment with L and with E produces an improvement in EC of similar magnitude. These changes are accompanied by a reshift of MHCs of leg skeletal muscle toward the slow, more fatigue-resistant isoforms. Magnitude of MHC1 changes correlates with the net peak V(O2) gain, which suggests that improved EC may be caused by favorable biochemical changes occurring in the skeletal muscle. 相似文献
70.
Luigi Bardelli Giacomo Poggi 《Nuclear instruments & methods in physics research. Section A, Accelerators, spectrometers, detectors and associated equipment》2006,560(2):517-523
The use of fast digital sampling techniques in Nuclear Physics experiments as a replacement of the standard analog signal processing methods is discussed for applications needing high-resolution signal amplitude measurements. This is for example the case of a solid-state detector with a charge-sensitive preamplifier, processed using fast digital sampling methods. Under very general assumptions, an expression for the achievable resolution and dynamic range of the system is reported, valid for any detector/digitizer/digital-filter combination, taking into account the detector noise and the ADC properties, namely the Effective Number of Bits (ENOB) and the sampling frequency. The system properties are summarized using the parameter PSENOB, i.e. the “Peak-Sensing-Equivalent Number of Bits”. These results can be used to predict the attainable performances in various applications, possibly requiring a resolution/dynamic-range trade-off. Numerical examples for some representative cases in γ-ray spectroscopy and charged particle experiments are reported, demonstrating that the equivalent performances of a 15 bit peak-sensing ADC are feasible with today-available sampling ADCs. For ease of presentation, other non-trivial effects as baseline- and non-linearity-related issues as well as experimental tests of the proposed approach are presented in a companion paper [L. Bardelli, G. Poggi, Digital sampling-systems in high-resolution and wide dynamic-range energy measurements: finite time window, baseline effects, and experimental tests, this issue]. 相似文献