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C D Perchonock I Uzinskas T W Ku M E McCarthy W E Bondinell B W Volpe J G Gleason B M Weichman R M Muccitelli J F DeVan 《Prostaglandins》1985,29(1):75-81
A series of desamino-2-nor-leukotriene analogs has been prepared by the reaction of various thiols with several methyl trans-4,5-epoxy-6Z-alkenoates, followed by deprotection. The products were assessed for their ability to antagonize the LTD4-induced contraction of the isolated guinea pig trachea. Several compounds displayed potent leukotriene antagonist activity, i.e., KB values in the sub-micromolar range, while only minimally affecting basal airway tone. The most potent analog, 4-hydroxy-5-(2-carboxyethylthio)-6Z-nonadecenoic acid, antagonized both LTD4- and LTE4-induced contractions of the trachea in an apparently competitive fashion. These agents possess increased potency relative to SK&F 101132, the first leukotriene analog identified as having LT-antagonist activity. Thus, these results demonstrate that deletion of the peptide amino group can produce leukotriene analogs which have minimal intrinsic contractile activity on the isolated guinea pig trachea, yet possess potent leukotriene-antagonistic effects. 相似文献
13.
Bonnie J. Reger Maurice S.B. Ku Jeffrey W. Pottert John J. Evans 《Phytochemistry》1983,22(5):1127-1132
The ribulose-1,5-bisphosphate carboxylase/oxygenase purified from maize (a C4 monocot) to homogeneity has a MW of532 000 and sedimentation coeffici 相似文献
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Š. Kužela 《Folia microbiologica》1969,14(1):77-81
The induced synthesis of β-galactosidase in non-growing cells ofEscherichia coli starving for exogenous carbon and nitrogen sources was stimulated markedly by the addition of any of four nucleosides tested: adenosine, guanosine, cytidine, and uridine. Adenosine was used as a representative of this group of compounds in most experiments. The decrease of ability of the cells to synthesize β-galactosidase, resulting from a prolonged starvation for exogenous carbon and nitrogen, was removed by adenosine. This compound also considerably reduced the inhibitory effect of metabolic poisons on the induced synthesis of β-galactosidase. The blockade of induced β-galactosidase synthesis evoked in aerobically grown cells by anaerobic starvation for exogenous sources of carbon and nitrogen was also significantly reduced by adenosine. The weak transient catabolic repression of induced synthesis of β-galactosidase evoked by glucose in non-growing cells ofEscherichia coli deprived of exogenous carbon and nitrogen sources was prevented by adenosine. The total repression caused by higher glucose concentrations was not influenced by this compound. The results are discussed from the point of view of the role of the energy state ofEscherichia coli cells in the regulation of β-galactosidase synthesis. 相似文献
17.
Vanadium was determined by radiochemical neutron activation analysis (RNAA) with proven accuracy in urine of workers occupationally
exposed to vanadium-rich dust in a vanadium pentoxide production plant, and values in the range of 3.02–762 ng/mL (median
33.0 ng/mL) were found. In a control group consisting of administrative workers of the plant, urinary vanadium levels were
found in the range of 1.05–53.4 ng/mL (median 2.53 ng/mL), whereas in an another control group of occupationally nonexposed
persons, these values amounted to 0.066–0.489 ng/mL (median 0.212 ng/mL).
Accuracy of the results was tested by analysis of reference material IAEA A-13 Animal Blood and NIST SRM-1515 Apple Leaves,
and very good agreement was found with literature and the NIST certified values, respectively. Unlike urine, no significant
differences were found for cystine levels in fingernails and hair of exposed and control persons. 相似文献
18.
Summary Ubiquinone-10 (Q10) production was measured in batch cultures of Paracoccus denitrificans grown for 8 h at increasing oxygen concentrations (0–21 % O2 in the sparging gas). Whereas the cellular level of Q10 decreased monotonically from 1.2 to 0.5 mol/g d.w., the total yield of Q10 was maximal at 2.5 % O2 and amounted to 350 nmol (0.3 mg) per L of culture. 相似文献
19.
H. Yasemin Yenilmez Nazli Farajzadeh Nilgün Güler Kuşçulu Dilek Bahar Sadin Özdemir Gülşah Tollu Mithat Güllü Zehra Altuntaş Bayır 《化学与生物多样性》2023,20(4):e202201167
In this study, three new axially disubstituted silicon phthalocyanines ( SiPc1–3 ) and their quaternized phthalocyanine derivatives ( QSiPc1–3 ) were prepared and characterized. The biological properties (antioxidant, antimicrobial, antibiofilm, and microbial cell viability activities) of the water-soluble silicon phthalocyanines were examined, as well. A 1 % DMSO diluted with pure water was used as a solvent in biological activity studies. All the compounds exhibited high antioxidant activity. They displayed efficient antimicrobial and antimicrobial photodynamic therapeutic properties against various microorganisms, especially Gram (+) bacteria. Additionally, they demonstrated high antibiofilm activities against S. aureus and P. aeruginosa. In addition, 100 % bacterial reduction was obtained for all the studied phthalocyanines against E. coli viable cells. Besides, the DNA cleavage and binding features of compounds ( QSiPc1–3 ) were studied using pBR322 DNA and CT-DNA, respectively. Furthermore, the human topoisomerase I enzyme inhibition activities of compounds QSiPc1 – 3 were studied. Anticancer properties of the water-soluble compounds were investigated using cell proliferation MTT assay. They exhibited anticarcinogenic activity against the human colon cancer cell line (DLD-1). Compounds QSiPc1 and QSiPc3 displayed a high anticarcinogenic effect on the DLD-1 cell line. The obtained results indicated that all the studied compounds may be effective biological agents and anticancer drugs after further investigations. 相似文献
20.
David D. Ku 《Life sciences》1982,30(3):277-284
The effects of chronic reserpine pretreatment (0.1 mg/kg/day, 7–9 days) on myocardial sodium pump activity, the binding of 3H-ouabain to Na+, K+-ATPase, and the positive inotropic effect of ouabain were studied in guinea pig hearts. Ouabain-sensitive 86Rb uptake, an estimate of sodium pump activity, was significantly decreased (33.0%) in papillary muscles of chronic reserpine-pretreated guinea pigs as compared to the saline-treated controls. Kinetic analyses of the interaction of 3H-ouabain with Na+, K+-ATPase indicated that chronic reserpine pretreatment resulted in a significant decrease (24.3%) in the maximum 3H-ouabain binding site concentration when the results were expressed as pmoles per mg protein. The maximum 3H-ouabain binding sites or the number of Na+, K+-ATPase units, however, were not significantly different between the two groups when they were expressed as pmoles per mg DNA. The affinity or the dissociation rate constant (Kd) of 3H-ouabain binding was not altered after chronic reserpine pretreatment. In isolated, electrically-driven left atrial preparations, the basal contractile force was slightly higher in the reserpine-pretreated animals; the subsequent development of the positive inotropic effect and the concentration of ouabain needed to produce half-maximal inotropic response, however, were not different from the controls. Thus, it is concluded that chronic reserpine pretreatment is accompanied by a significant reduction in myocardial sodium pump activity; however, the number of sodium pump sites per cell was unchanged. The sensitivity of the reserpine-pretreated myocardium to the inotropic action of ouabain as well as its affinity for 3H-ouabain binding are also unchanged. 相似文献