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81.
Stable Peptides Instead of Stapled Peptides: Highly Potent αvβ6‐Selective Integrin Ligands
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Dr. Oleg V. Maltsev Dr. Udaya Kiran Marelli Tobias G. Kapp Dr. Francesco Saverio Di Leva Dr. Salvatore Di Maro Dr. Markus Nieberler Prof. Dr. Ute Reuning Prof. Dr. Markus Schwaiger Prof. Dr. Ettore Novellino Prof. Dr. Luciana Marinelli Prof. Dr. Horst Kessler 《Angewandte Chemie (International ed. in English)》2016,55(4):1535-1539
The αvβ6 integrin binds the RGD‐containing peptide of the foot and mouth disease virus with high selectivity. In this study, the long binding helix of this ligand was downsized to an enzymatically stable cyclic peptide endowed with sub‐nanomolar binding affinity toward the αvβ6 receptor and remarkable selectivity against other integrins. Computational studies were performed to disclose the molecular bases underlying the high binding affinity and receptor subtype selectivity of this peptide. Finally, the utility of the ligand for use in biomedical studies was also demonstrated here. 相似文献
82.
Cristina M. Belfiore Mauro F. La Russa Luciana Randazzo Giuseppe Montana Antonino Pezzino Silvestro A. Ruffolo Piergiorgio Aloise 《Applied Physics A: Materials Science & Processing》2014,114(3):741-752
The present contribution is part of a biennial research project funded by the Italian Ministry of Education, Universities and Research (MIUR). This study, currently in progress, deals with innovative experimental approaches applied to the chemical, mineralogical and physical transformations occurring during the prolonged permanence of archaeological ceramic finds in seawater environments as well as to restoration and conservation issues of the same underwater artifacts. The experimental approach used in this research consisted in the manufacture of ceramic test-pieces (briquettes) and their successive placing in underwater environment. This work aims at assessing how textural and compositional parameters along with firing temperatures of a ceramic paste could affect total porosity, pore size distribution and kinetics of capillary water absorption. A further purpose is concerned with the study of the potential modification of porosity and pore size distribution in the same ceramic bodies after immersion in seawater (3 and 6 months). The study was carried out using a multi-technique approach including investigations through polarized light microscopy (PLM), capillary water absorption test, mercury intrusion porosimetry (MIP) analyses and theoretical calculation of salt crystallization pressures. The obtained results show a different behavior of the six experimental pastes as a function of their compositional and textural features as well as pore size distribution and firing temperatures. These parameters, in various extents, have been found significantly influencing the kinetics of water absorption and the susceptibility of ceramic artifacts to salt crystallization processes, with important implications on conservation procedures needed before the musealization. 相似文献
83.
Ciminiello P Dell'Aversano C Dello Iacovo E Fattorusso E Forino M Grauso L Tartaglione L Guerrini F Pezzolesi L Pistocchi R Vanucci S 《Journal of the American Chemical Society》2012,134(3):1869-1875
Since 2005, the benthic dinoflagellate Ostreopsis cf. ovata has bloomed across the Mediterranean basin, provoking serious toxic outbreaks. LC/MS studies have identified a number of palytoxin-like compounds, termed ovatoxins, along with trace amounts of putative palytoxin as the causative agents of the O. cf. ovata -related human sufferings. So far, any risk assessment for ovatoxins as well as establishment of their allowance levels in seafood has been prevented by the lack of pure toxins. The present paper reports on the isolation, NMR-based structural determination, and preliminary mouse lethality evaluation of ovatoxin-a, the major toxic compound contained in O. cf. ovata extracts. Availability of pure ovatoxin-a will open the double prospect of fully evaluating its toxicity and preparing reference standards to be employed in LC/MS quantitative analyses. Elucidation of ovatoxin-a's complex structure will ultimately herald the understanding of the molecular bases of ovatoxins bioactivity. 相似文献
84.
Alessandro Massella Giulia D'Intino Mercedes Fernández Sandra Sivilia Luca Lorenzini Silvia Giatti Roberto C Melcangi Laura Calzà Luciana Giardino 《BMC neuroscience》2012,13(1):12
Background
Multiple sclerosis (MS) varies considerably in its incidence and progression in females and males. In spite of clinical evidence, relatively few studies have explored molecular mechanisms possibly involved in gender-related differences. The present study describes possible cellular- and molecular-involved markers which are differentially regulated in male and female rats and result in gender-dependent EAE evolution and progression. Attention was focused on markers of myelination (MBP and PDGFαR) and neuronal distress and/or damage (GABA synthesis enzymes, GAD65 and GAD67, NGF, BDNF and related receptors), in two CNS areas, i.e. spinal cord and cerebellum, which are respectively severely and mildly affected by inflammation and demyelination. Tissues were sampled during acute, relapse/remission and chronic phases and results were analysed by two-way ANOVA. 相似文献85.
Santos AK Machado LL Bizerra AM Monte FJ Santiago GM Braz-Filho R Lemos TL 《Natural product communications》2012,7(6):729-730
A new indole alkaloid of the pyridocarbazole type, named 6N-hydroxy-olivacine, and two known compounds, 2N-oxide-olivacine and olivacine, were isolated from roots of Peschiera affinis. The structures of the compounds were determined by spectroscopic {IR and extensive NMR (COSY, HMQC, HMBCand NOESY)} and EIMS analysis. 相似文献
86.
dos Anjos JV Srivastava RM Costa-Silva JH Scotti L Scotti MT Wanderley AG Leite ES de Melo SJ Mendonça Junior FJ 《Molecules (Basel, Switzerland)》2012,17(1):809-819
In this study, the antinociceptive properties of 3,4-dihydro-2,6-diaryl-4-oxo-pyrimidine-5-carbonitrile derivatives 5a-i at doses of 25 and 50 mg/kg were evaluated in mice, using the abdominal constriction test. Molecular modeling studies were also performed using density functional theory calculations. These data provided information about the electrostatic and ionization potentials and were used to compare the antinociceptive activity of the title compounds. The most active compounds were 3,4-dihydro-2-(4-chlorophenyl)-6-(4-methoxyphenyl)-4-oxo-pyrimidine-5-carbonitrile (5b) and 3,4-dihydro-2,6-diphenyl-4-oxo-pyrimidine-5-carbonitrile (5i), which inhibited the number of abdominal constrictions, at 50 mg/kg dose, in 88.6% and 88% of the sample, respectively. A preliminary SAR study demonstrated that halogen replacement in the phenyl rings of the compounds under study reduces the antinociceptive activity. DFT calculations showed that there is a high correlation between the ionization potentials and the analgesic properties of the compounds. It was found that compounds with a positive ionization potential (compounds 5b and 5i) were found to be the best analgesic drugs in this series. 相似文献
87.
Formation of inclusion complexes and controlled release of atrazine using free or silica-anchored β-cyclodextrin 总被引:1,自引:0,他引:1
Lucas Bragan?a de Carvalho Luciana de Matos Alves Pinto 《Journal of inclusion phenomena and macrocyclic chemistry》2012,74(1-4):375-381
Immobilization of cyclodextrin on the surface of silica was performed using citric acid as the bonding agent. Inclusion complexes of atrazine with free (CD) or anchored (CDSI) β-cyclodextrin were prepared and then characterized using infrared spectroscopy, X-ray diffraction and differential scanning calorimetry. The complexation reaction showed first order kinetics, with a rate constant (k) of 8.72?×?10?3 min?1. There was a rapid increase of absorbance in the first 40?min, followed by attainment of equilibrium after ~2?h. The stoichiometry of the reaction was 1:1, with both free and anchored β-cyclodextrin increasing the solubilization of atrazine in an aqueous medium (by around 1.5 and 3.4 times, respectively). The association constant (K a) of the complex was 28.93?L?mol?1 using CD and 130.68?L?mol?1 using CDSI. In release tests, 62% of the atrazine complexed with CDSI or β-CD was released after 40?h, while 83% of free atrazine was released during the same period. 相似文献
88.
Gonçalves Luciana R. B. Suzuki Glória S. Giordano Roberto C. Giordano Raquel L. C. 《Applied biochemistry and biotechnology》2001,91(1-9):691-702
Applied Biochemistry and Biotechnology - Kinetic and mass transport parameters were estimated for maltotriose hydrolysis using glucoamylase immobilized on macroporous silica and wrapped in pectin... 相似文献
89.
Giordano Raquel L. C. Hirano Paulo C. Gonçalves Luciana R. B. Netto Willibaldo Schmidell 《Applied biochemistry and biotechnology》2000,84(1-9):643-654
This article presents a detailed study on the conditions for achieving a stable biocatalyst to be used in the production of
ethanol from starch. Different pellets were used depending on which characteristic of the biocatalyst was being studied: (a)
Saccharomyces cerevisiae entrapped in pectin or calcium alginate gel particles; (b) silica containing immobilized glucoamylase entrapped in pectin
gel particles; or (c) pectin gel particles, with the silicaenzyme derivative and yeast coimmobilized. The influence of several
variables on the mechanical resistance of the particle, on the viability of the microorganism, and on the rate of substrate
hydrolysis was studied with biocatalyst. The best conditions found were 6% pectin gel, 2-mm particle diameter, and curein
0.2 M CaCl2·2H2O/60 mM acetate buffer, pH 4.2, for gel preparation; and 6.0 g/L of CaCl2·2H2O in the fermentation medium. Biocatalyst (c) was successfully tested for the production of ethanol from liquefield manioc
flour syrup. 相似文献
90.
Maurizio Penco Luciana Sartore Stefania Della Sciucca Luca Di Landro Alberto D'Amore 《Macromolecular Symposia》2007,247(1):252-259
In this work the effect of melt mixing condition and of a trans-esterification catalyst on miscibility of poly(methyl methacrylate) (PMMA)/polycarbonate of bisphenol A (PC) blends is studied. In particular, at high temperature chemical reactions between PMMA and PC phases can take place; these strongly change the compatibility in the blend and materials having single Tg can be obtained. FT-IR analyses, coupled with solvent extraction, suggest that a grafting reaction of PC on PMMA is involved. SEC and DSC data are consistent with spectroscopic results, and some decrement of the molar weight distribution (MWD) of PC phase is observed. On the other hand, the presence of a fraction of modified material having higher MWD of starting PMMA is also noticed. The single Tg characteristic of some materials has been confirmed by experimental data of structural relaxation performed by differential scanning calorimetry (DSC). These materials showed optical clarity and the morphological analysis performed by scanning electron microscopy (SEM) confirm the homogeneity of these materials. 相似文献