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71.
A procedure is described in which gold(III) is quantitatively extracted with an amidine into chloroform over the acidity range pH 3.0–11.0 M HCl, followed by its selective spectrophotometric determination by interaction of the extract with methylene blue in the pH range 3.0–9.0. The molar absorptivity of the coloured complex formed by extraction with ten different amidines and methylene blue reaction lie in the range 1.1 × 104?6.5 × 104 1 mol?1 cm?1 at λmax (650 nm) in chloroform. The simplest compound, N, N′-diphenylbenzamidine, was chosen for detailed study. The limit of detection is 5 μg Au l?1. The method is free from interferences from the metals that are generally associated with gold. The method is simple, reproducible and applicable to the accurate recovery of gold from low-grade ores containing the metal at levels of > 1.5 μg g?1.  相似文献   
72.
A new fragment-based method for the rapid development of novel and distinct classes of nonpeptidic protease inhibitors, Substrate Activity Screening (SAS), is described. This method consists of three steps: (1) a library of N-acyl aminocoumarins with diverse, low molecular weight N-acyl groups is screened to identify protease substrates using a simple fluorescence-based assay, (2) the identified N-acyl aminocoumarin substrates are optimized by rapid analogue synthesis and evaluation, and (3) the optimized substrates are converted to inhibitors by direct replacement of the aminocoumarin with known mechanism-based pharmacophores. The SAS method was successfully applied to the cysteine protease cathepsin S, which is implicated in autoimmune diseases. Multiple distinct classes of nonpeptidic substrates were identified upon screening an N-acyl aminocoumarin library. Two of the nonpeptidic substrate classes were optimized to substrates with >8000-fold improvements in cleavage efficiency for each class. Select nonpeptidic substrates were then directly converted to low molecular weight, novel aldehyde inhibitors with nanomolar affinity to cathepsin S. This study demonstrates the unique characteristics and merits of this first substrate-based method for the rapid identification and optimization of weak fragments and provides the framework for the development of completely nonpeptidic inhibitors to many different proteases.  相似文献   
73.

A convenient methodology has been developed for the synthesis of glycosylenaminoesters directly from glycosyl azides under hydrogenation conditions. Yields were moderate to good in all cases.  相似文献   
74.
Russian Journal of Organic Chemistry - A simple, green, and efficient protocol has been developed for the synthesis of biologically active 1,4dihydropyrano[2,3c]pyrazole derivatives via one-pot...  相似文献   
75.
High Energy Chemistry - Recent reports on nanoparticles rise significantly as they possess numerous applications in medical, material science, optics, and bioscience etc. Nanoparticles show unique...  相似文献   
76.
Antimicrobial properties casing wide applicability in water detoxification, pharmaceutics and in industries. Present work focus on the synthesis of a new series of Schiff Bases (E)-4-(1 substituted-1H Benzo[d]imidazole-2-yl)-N'-(substituted Benzylidene)benzohydrazide (5a-5l) were synthesized. The convenient route for the synthesis of new analogues by the condensation of 4-(substituted -1H-Benzo[d]imidazole-2-yl)-N'- Hydrazine with different derivatives of aromatic aldehydes were described using different solvents and catalysts. The structures of the synthesized compounds were ascertain by spectral techniques viz. IR, 1H NMR, MS and Physical Elemental data. Compounds were also subjected to thermal analysis to study their physical and chemical properties. The title compounds were also screened for their antimicrobial activity against various bacterial & Fungal strains. Results of bioassay vary with diverse group attached to Benzimdazole motif and could be helpful for the development of other bioactive molecules.  相似文献   
77.
Amide and ester conjugates of aceclofenac with polyamidoamine (PAMAM-G0) dendrimer zero generation and dextran (40 kDa) polymeric carrier, respectively, are presented. The prepared conjugates were characterized by UV, TLC, HPLC, IR, and 1H NMR spectroscopy. The average degrees of substitution of amide and ester conjugates were determined and found to be (12.5 ± 0.24) % and (7.5 ± 0.25) %, respectively. The in vitro hydrolysis studies showed that dextran ester conjugate hydrolyzed faster in a phosphate buffer solution of pH 9.0 as compared to PAMAM dendrimer G0 amide conjugate, and followed the first order kinetics. No amount of the drug was regenerated at pH 1.2 in simulated gastric fluid. The dextran conjugate showed short half-life as compared to the PAMAM dendrimer conjugate. Anti-inflammatory and analgesic activities of the dendrimer conjugate were found to be similar to those of the standard drug. Results of chronic ulceroginic activity showed deep ulceration and high ulcer index for aceclofenac, whereas lower ulcer index was found for the PAMAM dendrimer and dextran (40 kDa) conjugates. Experimental data suggest that PAMAM dendrimer and dextran (40 kDa) can be used as carriers for the sustained delivery of aceclofenac along with a remarkable reduction in gastrointestinal toxicity.  相似文献   
78.
The results of photoconductivity (PC), photoluminescence (PL), optical absorption spectra, XRD and SEM studies are presented for (Cd0.95-Pb0.05)S: CdCl2,Ce films prepared by chemical bath deposition technique. PC gains ∼107 are found in doped films. PL emission spectrum is found in red region which is related to 5d to 4f transition in Ce. Films prepared at 60°C show better PC while those prepared at room temperature (RT) show better PL. Optical absorption studies show reduction in band gap due to addition of PbS. A peak due to Ce is also observed in absorption spectrum. XRD studies show the presence of both CdS and PbS. SEM studies show presence of microcrystals, cluster of grains along with some rod type structures.  相似文献   
79.
An enzymatic method for the determination vitamin A (retinol) is reported using soluble and immobilized alcohol dehydrogenase, isolated from rabbit liver. The reaction is based on the oxidation of retinol and simultaneous reduction of NAD+ to NADH followed by spectrophotometric detection at 340 nm. The calibration graph was linear over the range of 2.0–10 μM with correlation coefficients of 0.9967 and 0.9992 (n = 5) for soluble and immobilized alcohol dehydrogenase respectively, with relative standard deviations (n = 3) in the range of 0.5–1.2%. The limit of detection was lower than 1.0 μM. The proposed method was applied to determine vitamin A in pharmaceuticals, and the results obtained were in reasonable agreement with the amount labeled. The results were compared using spectrophotometric reference method, and no significant difference was found between the results of the both methods.  相似文献   
80.
An amino‐acid‐based hydrophobically modified biocompatible copolymer, poly[(sodium N‐acryloyl‐L ‐valinate)‐co‐(N‐octylacrylamide)] was synthesized and characterized. Techniques such as fluorescence probes, DLS, and TEM were used to investigate its aggregation behavior in aqueous solution. The copolymer was observed to form micellar aggregates having diameters in the nanometer range in aqueous solution (pH = 8) through inter‐chain hydrophobic association. This behavior was found to be similar to that of poly[(sodium N‐acryloyl‐L ‐valinate)‐co‐(N‐dodecylacrylamide)]. The compact micellar nanostructures were observed to be stable with respect to changes of pH and temperature. The encapsulation and release of griseofulvin, a hydrophobic model drug, was studied.

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