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991.
Rapid screening of membrane protein activity: electrophysiological analysis of OmpF reconstituted in proteoliposomes 总被引:1,自引:0,他引:1
Solvent-free planar lipid bilayers were formed in an automatic manner by bursting of giant unilamellar vesicles (GUVs) after gentle suction application through micron-sized apertures in a borosilicate glass substrate. Incubation of GUVs with the purified ion channel protein of interest yielded proteoliposomes. These proteoliposomes allow for immediate recording of channel activity after GUV sealing. This approach reduces the time-consuming, laborious and sometimes difficult protein reconstitution processes normally performed after bilayer formation. Bilayer recordings are attractive for investigations of membrane proteins not accessible to patch clamp analysis, like e.g. proteins from organelles. In the presented work, we show the example of the outer membrane protein OmpF from Escherichia coli. We reconstituted OmpF in proteoliposomes and observed the characteristic trimeric conductance levels and the typical gating induced by pH and transmembrane voltage. Moreover, OmpF is the main entrance for beta-lactam antibiotics and we investigated translocation processes of antibiotics and modulation of OmpF by spermine. We suggest that the rapid formation of porin containing lipid bilayers is of potential for the efficient electrophysiological characterization of the OmpF protein, for studying membrane permeation processes and for the rapid screening of antibiotics. 相似文献
992.
Nouria A. Al-Awadi Maher R. Ibrahim Ismail A. Abdelhamid Mohamed H. Elnagdi 《Tetrahedron》2008,64(35):8202-8205
Arylhydrazonals were added to acrylonitrile or methyl vinyl ketone in the presence of DABCO or benzotriazole to yield the intermediate Baylis-Hillman adduct that cyclized under the reaction conditions with water elimination to yield dihydropyridazines. A pyridazine reacted with DMAD to yield a pyridine via a [4+2] Diels-Alder addition followed by retro Diels-Alder elimination of methylene aniline. Two pyridazines were condensed with DMFDMA to yield the corresponding enaminones that reacted with NH2NH2 to afford the pyrazolylpyridazines. 相似文献
993.
Palladium catalyzed cross-coupling of 3-amino- and 3-acylamido-2-bromopyridines 1a-f with triethyl phosphite allowed the synthesis of 3-amino- and 3-acylamido pyridine-2-phosphonic acid diethyl esters 2a-f, whereas nickel catalysts, although providing access to related anilido-2-phosphonates, proved inactive. Reduction of the aminophosphonate 2a with LiAlH4 afforded 3-amino-2-phosphinopyridine (3a), which was cyclocondensed with dimethylformamide dimethyl acetal (DMFA) via phosphaalkene intermediates 4a to the novel pyrido[b]-anellated 1,3-azaphosphole 5a. Reaction of amidophosphonates 2b-f with LiAlH4 did not result in the expected reductive cyclization, as shown by closely related anilido-2-phosphonates, but led to product mixtures containing N-secondary 3-amino-2-phosphinopyridines 3b-f as the main or major component. The conversion of 3b,d,e with DMFA to 5b,d,e provides first examples of N-substituted pyrido[b]-anellated azaphospholes. Structures were confirmed by multinuclear NMR and X-ray crystallography (for 2c, 3b). 相似文献
994.
Mohamed Salah K. Youssef Ragaa A. Ahmed Mohamed S. Abbady Shawkat A. Abdel-Mohsen Ahmed A. Omar 《Monatshefte für Chemie / Chemical Monthly》2008,45(8):553-559
4-(2-Aminothiazol-4-yl)-3-methyl-5-oxo-1-phenyl-2-pyrazoline was synthesized via the reaction of 4-bromoacetyl-3-methyl-5-oxo-1-phenyl-2-pyrazoline with thiourea [7] and was transformed to related fused
heterocyclic systems. The antifungal and antibacterial studies revealed in some cases excellent biocidal properties. 相似文献
995.
Emad M. El-Telbani Mohamed F. El Shehry Galal A. M. Nawwar 《Monatshefte für Chemie / Chemical Monthly》2008,387(2):685-689
Synthesis of the title ring system is described using ethyl 4-(2,4-dichlorophenoxy)-3-oxobutanoate as starting material. The
latter was prepared through acylating Meldrum’s acid with the phenoxy acid chloride derivative. 相似文献
996.
Summary. Several derivatives of 5-arylmethylenebis(1-methyl-6-amino-2-thiouracils) and 5-aryldipyrimidopyridines were prepared by stirring
of 6-amino-1-methyl-2-thiouracil and 6-amino-1-benzyluracil with different aromatic aldehydes in ethanol in the presence of
HCl or refluxing with AcOH. On the other hand, 6-alkylthio-3,9-dimethylpurine-2-ones were synthesized by the alkylation of 3,9-dimethyl-6-thioxanthine
which was prepared by treatment of 3,9-dimethylxanthine with P2S5. The structures of the novel compounds were characterized by spectroscopic methods. The effects of the novel compounds on
both HAV and HSV type 1 were investigated. Also, some compounds showed inhibitory effects on Gram-positive and Gram-negative bacteria as well as yeast and fungi.
On leave from Chemistry Department, Faculty of Science, Zagazig University, Zagazig, Egypt 相似文献
997.
Bakr F. Abdel-Wahab Salwa F. Mohamed Abd El-Galil E. Amr Mohamed M. Abdalla 《Monatshefte für Chemie / Chemical Monthly》2008,139(9):1083-1090
Methyl 2-(thiazol-2-ylcarbamoyl)acetate was synthesized and used as starting material. It was treated with hydrazine hydrate
to afford the hydrazide, which was reacted with nitromethane and formaldehyde to give the saturated nitropyrimidine. The hydrazide
was reacted with phenyl isothiocyanate to afford the thiosemicarbazide, which was cyclized with ethyl bromoacetate, sodium
hydroxide, or sulfuric acid to afford N-phenylthiazolidinone, N-phenyltriazole, and thiadiazolyl derivatives. The methyl 2-(thiazol-2-ylcarbamoyl)acetate was coupled with diazonium salts
of aniline, 4-chloroaniline, 4-bromoaniline, or 4-aminobenzenesulfonamide to afford the carbamoyl acetates, which were reacted
with 2-aminobenzimidazole, 1,2,4,5-tetrachlorophthalic anhydride, and hydrazine hydrate to afford the corresponding thiazolylmalonamide,
tetrachloroisoindolylimide, and tri-azole derivatives. Schiff bases and imides are newly synthesized candidates obtained via simple condensation of the hydrazide with aldehydes, 2,3-pyridinedicarboxylic anhydride, or 1,8-naphthalenedicarboxylic anhydride.
The pharmacological screening showed that many of these compounds have good antihypertensive α-blocking activity and low toxicity.
Correspondence: Abd El-Galil E. Amr, National Research Center, Applied Organic Chemistry, Dokki, Cairo, Egypt. 相似文献
998.
Samir Bondock Hossam El-Azap Ez-Eldin M. Kandeel Mohamed A. Metwally 《Monatshefte für Chemie / Chemical Monthly》2008,139(11):1329-1335
Highly versatile ethyl 3-thiosemicarbazidobutanoate was ball-milled with phenacyl bromide to afford the corresponding ethyl
3-[(4-phenyl-2-thiazolyl)hydrazono]butanoate which underwent heterocyclization by heating in ethanolic sodium acetate to give
thiazolylpyrazolone that coupled chemoselectively with aromatic diazonium salts to furnish arylhydrazonothiazolylpyrazoles.
Vilsmeier-Haack reaction of ethyl 3-thiosemicarbazidobutanoate furnished selectively thiazolylpyrazole. A series of pyrazolylthiosemicarbazones
were synthesized by solid-state technique which allowed waste-free production. The reaction of pyrazolylthiosemicarbazones
with phenacyl bromide afforded the corresponding 2-(arylidenehydrazino)-4-phenylthiazoles in quantitative yields.
Correspondence: Samir Bondock, Department of Chemistry, Faculty of Science, Mansoura University, ET-31556 Mansoura, Egypt. 相似文献
999.
Mohamed M. Abdulla 《Monatshefte für Chemie / Chemical Monthly》2008,139(6):697-705
A series of pyridines, pyrimidinone, oxazinones, and their derivatives were synthesized as anti-inflammatory agents using abietic acid (7-isopropyl-1,4a-dimethyl-1,2,3,4,4a,4b,5,6,10,10a-decahydrophenanthrene-1-carboxylic acid) as the starting material. The arylidiene derivative was treated with cyanothioacetamide to give cyano pyridine-thione, which was reacted with ethyl chloroacetate to yield the corresponding cyano ester. The ester was hydrolysed to the sodium salt, which was reacted with acetic anhydride to afford 2-methyloxazinone, which was treated with ammonium acetate to afford 2-methylpyrimidinone followed by methylation with methyl iodide to yield 2,3-dimethyl- pyrimidinone. In addition, the oxazinone derivative was reacted with aniline or hydrazine hydrate to give 3-phenyl- or 3-aminopyrimidinones. The latter reacted with thiophene-2-carboxaldehyde or phenylisothiocyanate to afford Schiff’s bases or thiosemicarbazide derivatives. The pharmacological screening showed that many of these compounds have good anti-inflammatory activity comparable to Prednisolone® as reference drug. 相似文献
1000.
Victor Mamane Frédéric Louërat Julien Iehl Mohamed Abboud Yves Fort 《Tetrahedron》2008,64(47):10699-10705
A new, short and efficient synthesis of substituted benzo-(iso)quinoline derivatives is reported. The methodology is based on a Suzuki or Negishi cross-coupling followed by a cyclization reaction induced by t-BuOK in DMF to form the central ring. This approach allowed the synthesis of all four benzo-(iso)quinoline isomers and the substitution of each ring of the benzo-(iso)quinoline core. 相似文献