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661.
662.
Feliciana Real-Fernández Francesca Nuti M. Angeles Bonache Marco Boccalini Stefano Chimichi Mario Chelli Anna Maria Papini 《Amino acids》2010,39(2):599-604
The synthesis of N-protected glycosyl amino acids from amines has been investigated and it was found that, under microwave conditions, glycosylamines
could be hydrolyzed leading to new products containing a glycosyl ester linkage. The efficiency of the microwave-induced glycosylation
of aspartic acid was studied comparing the microwave activity between amide and ester bond formation. Different sugar moieties
have been employed to demonstrate the simple and reproducible coupling methodology. New glycosyl ester compounds were further
characterized by NMR spectroscopy. 相似文献
663.
Thalita G. Barros Sergio Pinheiro J. S. Williamson Amílcar Tanuri M. Gomes Jr Helena S. Pereira R. M. Brindeiro José B. A. Neto O. A. C. Antunes Estela M. F. Muri 《Amino acids》2010,38(3):701-709
In this paper, we describe the synthesis of a novel class of pseudo-peptides derived from isomannide and several oxazolones as potential inhibitors of serine proteases as well as preliminary pharmacological assays for hepatitis C. Hepatitis C, dengue and West Nile fever are among the most important flaviviruses that share one important serine protease enzyme. Serine proteases belong to the most studied class of proteolytic enzymes and are a primary target in the drug development field. Several pseudo-peptides were obtained in good yields from the reaction of isomannide and oxazolones, and their anti-HCV potential using the HCV replicon-based assay was shown. 相似文献
664.
The N-tosyl carbamates 4a–e, easily prepared starting from the Baylis–Hillman adducts 3a–e, underwent cyclization carried out with I2/NIS in the presence of NaH, to give the corresponding 2-oxo-1,3-oxazolidines 5a–e in good yield and total stereoselection when the substituent at C-5 is Ar. After the removal of tosyl group, followed by
the cleavage of the heterocyclic ring, the α-methyl-α-amino acids 8a,b and 10 were obtained in good yield as hydrochlorides. 相似文献
665.
Jared J. Heymann Mario Gabričević Timothy A. Mietzner Alvin L. Crumbliss 《Journal of biological inorganic chemistry》2010,15(2):237-248
The bacterial transferrin ferric binding protein A (FbpA) requires an exogenous anion to facilitate iron sequestration, and
subsequently to shuttle the metal across the periplasm to the cytoplasmic membrane. In the diverse conditions of the periplasm,
numerous anions are known to be present. Prior in vitro experiments have demonstrated the ability of multiple anions to fulfill
the synergistic iron-binding requirement, and the identity of the bound anion has been shown to modulate important physicochemical
properties of iron-bound FbpA (FeFbpA). Here we address the kinetics and mechanism of anion exchange for the FeFbpA–nitrilotriacetate
(NTA) assembly with several biologically relevant anions (citrate, oxalate, phosphate, and pyrophosphate), with nonphysiologic
NTA serving as a representative synergistic anion/chelator. The kinetic data are consistent with an anion-exchange process
that occurs in multiple steps, dependent on the identity of both the entering anion and the leaving anion. The exchange mechanism
may proceed either as a direct substitution or through an intermediate FeFbpA–X* assembly based on anion (X) identity. Our
kinetic results further develop an understanding of exogenous anion lability in the periplasm, as well as address the final
step of the iron-free FbpA (apo-FbpA)/Fe3+ sequestration mechanism. Our results highlight the kinetic significance of the FbpA anion binding site, demonstrating a correlation
between apo-FbpA/anion affinity and the FeFbpA rate of anion exchange, further supporting the requirement of an exogenous
anion to complete tight sequestration of iron by FbpA, and developing a mechanism for anion exchange within FeFbpA that is
dependent on the identity of both the entering anion and the leaving anion. 相似文献
666.
Elíades Lorena Cabello Marta Voget Claudio Galarza Betina Saparrat Mario 《World journal of microbiology & biotechnology》2010,26(11):2105-2111
A screening was carried out on 69 fungal strains isolated from alkaline-calcareous, neutral and alkaline-sodic soils, as well
as from their associated plant material, to determine their ability to grow at alkaline pH. A total of 32 fungi were selected
for their ability to produce alkaline keratinase activity in submerged shaken cultures supplemented with soybean meal (SM)
and tryptone and on cow hair (CH) under solid state fermentation conditions. Although several fungal strains produced keratinolytic
activity on both SM and CH, they differed in the levels detected. Among them, Aspergillus niger, Cladosporium cladosporioides, Metarrhizium anisopliae, Neurospora tetrasperma and Westerdikella dispersa were the best producers, with levels higher than 1.2 U ml−1. Different fungal species are here reported for the first time for their ability to produce keratinolytic activity at alkaline
pH. 相似文献
667.
668.
Jan Svetlik Lucia Veizerová Thomas U. Mayer Mario Catarinella 《Bioorganic & medicinal chemistry letters》2010,20(14):4073-4076
A synthesis of novel pyrazolopyridine, benzopyranopyrazolopyridine, and oxygen-bridged pyrazolo-, tetrazolo-, benzimidazo-, and thiazolopyrimidines via Hantzsch- and Biginelli-like condensations has been developed. The ability of these compounds to inhibit Eg5 activity has been examined. The results indicate that synthetic manipulations in the monastrol thiourea moiety are inefficient. 相似文献
669.
Jiaqiang Cai D. Jonathan Bennett Zoran Rankovic Maureen Dempster Xavier Fradera Jonathan Gillespie Iain Cumming William Finlay Mark Baugh Sylviane Boucharens John Bruin Kenneth S. Cameron William Hamilton Jennifer Kerr Emma Kinghorn George McGarry John Robinson Paul Scullion Joost C.M. Uitdehaag Mario van Zeeland Eric Nicolai 《Bioorganic & medicinal chemistry letters》2010,20(15):4447-4450
Starting from previously disclosed equally potent cathepsin K and S inhibitor 4-propyl-6-(3-trifluoromethylphenyl)pyrimidine-2-carbonitrile 1, a novel 2-phenyl-9H-purine-6-carbonitrile scaffold was identified to provide potent and selective cathepsin S inhibitors. 相似文献
670.
Felipe F.D. Oliveira Diego C.B.D. Santos Alexandre A.M. Lapis José R. Corrêa Alexandre F. Gomes Fabio C. Gozzo Paulo F. Moreira Virgínia C. de Oliveira Frank H. Quina Brenno A.D. Neto 《Bioorganic & medicinal chemistry letters》2010,20(20):6001-6007
Newly designed 2,1,3-benzothiadiazole-containing fluorescent probes with four excited state intramolecular proton transfer (ESIPT) sites were successfully tested in live cell-imaging assays using a confluent monolayer of human stem-cells (tissue). All tested dyes were compared with the commercially available DAPI and gave far better results. 相似文献