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21.
Masatoshi Oue Akira Ishigaki Keiichi Kimura Yousuke Matsui Toshiyuki Shono 《Journal of polymer science. Part A, Polymer chemistry》1985,23(7):2033-2042
Poly- and bis(thiacrown ether) derivatives in which some oxygen atoms of benzocrown ether moiety are replaced by sulfur atoms have been synthesized. Their cation-binding abilities were investigated by using the solvent extraction method. The poly- and bis(benzothiacrown ether)s showed great affinity for silver ion, being more excellent in the affinity than the corresponding monocyclic analogs. They, however, possess very poor cation-binding ability for alkali and alkaline-earth metal ions. The poly- and bis(thiacrown ether)s also bind mercuric ions effectively, whereas the corresponding monomeric analogs do not at all. 相似文献
22.
S Ozaki T Akiyama T Morita M Kumegawa T Nagase N Uehara A Hoshi 《Chemical & pharmaceutical bulletin》1990,38(11):3164-3166
Various kinds of 5'-O-unsaturated acyl 5-fluorouridines were synthesized to obtain 5-fluorouridine derivatives with low toxicity and high antitumor activity. Antitumor activity of the compounds against L-1210 leukemia in mice was examined, and the 5'-O-4-pentenoyl derivative showed the highest antitumor activity. 相似文献
23.
K Yoshino K Goto T Kohno T Morita G Tsukamoto 《Chemical & pharmaceutical bulletin》1990,38(3):676-680
Various asymmetric or cyclic ester derivatives of the phosphonic acid moiety in the calcium antagonist fostedil (KB-944) were synthesized. The coronary vasodilator activity of these compounds was assessed by Langendorff's method. Among them, the ethyl isopropyl ester 12 showed the most potent activity, which was comparable to that of fostedil. 相似文献
24.
Antiviral activity of natural occurring flavonoids in vitro 总被引:2,自引:0,他引:2
Y Tsuchiya M Shimizu Y Hiyama K Itoh Y Hashimoto M Nakayama T Horie N Morita 《Chemical & pharmaceutical bulletin》1985,33(9):3881-3886
25.
Y Nishioka S Kyotani M Okamura M Miyazaki Y Sakamoto M Morita K Okazaki S Ohnishi Y Yamamoto K Ito 《Chemical & pharmaceutical bulletin》1992,40(1):267-268
Hepatic artery of dogs was embolized with cisplatin (CDDP) albumin microspheres containing chitin and chitosan to investigate the in vivo CDDP release kinetics from CDDP albumin microspheres, the CDDP cumulative characteristics in the liver, and the influence of microsphere administration on hepatic tissue. Results showed that changes in blood CDDP content were dependent on CDDP albumin microsphere type and that release kinetics were better sustained when chitin was added to the microspheres or when the microspheres were treated with chitosan. In particular, the administration of CDDP in the chitin-containing CDDP chitosan albumin microspheres showed a blood CDDP content of approximately 0.26 micrograms Pt/ml 14 d after administration. The administration of chitin-containing or chitosan treated CDDP microspheres showed a CDDP content in the hepatic tissue of 0.14 to 0.23 micrograms Pt/g 28 d after administration. They also showed better control of CDDP release than those without chitin or chitosan treatment. No CDDP influence on hepatic tissue was observed. We conclude that, even in vivo, chitin and chitosan are effective embolic materials. 相似文献
26.
The structure and stereochemistry of scopadulin, a novel aphidicolane-type diterpene isolated from Scoparia dulcis L. have been established from spectral data and single-crystal X-ray analysis of its acetone solvate. 相似文献
27.
T Morita F Mikami A Kanagawa M Sera H Ueki 《Chemical & pharmaceutical bulletin》1991,39(12):3287-3289
Vanadate stimulated the release of rat hepatic lipase activity from liver slices into an incubation medium in a time- and dose-dependent manner. Insulin, however, failed to have this stimulatory action, and the release by heparin was recognized, but was not additive to that by vanadate. Amiloride, an inhibitor of tyrosine kinase in some receptors and of the Na+/H+ exchange system suppressed the vanadate-stimulated release. Biochanin A, a different type of tyrosine kinase inhibitor than amiloride, also suppressed the effect of vanadate. The stimulation by vanadate was clearly preserved in Na(+)-, K(+)-, or Ca(2+)-free medium, suggesting that neither the Na+/H+ exchange system, Na+, K(+)-adenosine triphosphatase, nor Ca(2+)-influx into cells is involved in the action of this substance. These results suggest that vanadate-stimulated release of the enzyme activity is associated with the activation of the tyrosine kinase activity. 相似文献
28.
Evaluation of the disintegration time of rapidly disintegrating tablets via a novel method utilizing a CCD camera 总被引:6,自引:0,他引:6
Morita Y Tsushima Y Yasui M Termoz R Ajioka J Takayama K 《Chemical & pharmaceutical bulletin》2002,50(9):1181-1186
Many kinds of rapidly disintegrating or oral disintegrating tablets (RDT) have been developed to improve the ease of tablet administration, especially for elderly and pediatric patients. In these cases, knowledge regarding disintegration behavior appears important with respect to the development of such a novel tablet. Ordinary disintegration testing, such as the Japanese Pharmacopoeia (JP) method, faces limitations with respect to the evaluation of rapid disintegration due to strong agitation. Therefore, we have developed a novel apparatus and method to determine the dissolution of the RDT. The novel device consists of a disintegrating bath and CCD camera interfaced with a personal computer equipped with motion capture and image analysis software. A newly developed RDT containing various types of binder was evaluated with this protocol. In this method, disintegration occurs in a mildly agitated medium, which allows differentiation of minor distinctions among RDTs of different formulations. Simultaneously, we were also able to detect qualitative information, i.e., morphological changes in the tablet during disintegration. This method is useful for the evaluation of the disintegration of RDT during pharmaceutical development, and also for quality control during production. 相似文献
29.
Keiichiro Fukumoto Masatoshi Chihiro Yuichi Shiratori Masataka Ihara Tetsuji Kametani Toshio Honda 《Tetrahedron letters》1982,23(29):2973-2976
Thermolysis of a benzocyclobutene derivative () prepared from norcamphor produced stereoselectively a tetracyclic compound (), which was converted to a lactone () having correct stereochemistry at C7, C8, C9, C11, C13, and C14 positions of (±)-klaineanone. 相似文献
30.
Masatoshi Sakae Masanori Katsurada Mayumi Watanabe Fumio Yoneda Sadao Nishigaki Toshimasa Ishida 《Journal of heterocyclic chemistry》1997,34(1):157-160
The reaction of 2-bromoethylamine 1 with methylisothiocyanate 2 under mild condition gave 2-methyl-amino-2-thiazoline 3 as the major product together with two kinds of byproducts, 3-(N-methylthiocar-bamoyl)-2-methyliminothiazolidine 4 and N,N′-dimethyl-N-(2-thiazolin-2-yl)thiourea 5. Thermal isomer-ization of 5 to 4 was observed. The structures of the byproducts were confirmed by X-ray crystallography. 相似文献