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11.
Background
Existing cut-offs for fasting plasma glucose (FPG) and post-load glucose (2hPG) criteria are not equivalent in the diagnosis of diabetes and glucose intolerance. Adjusting cut-offs of single measurements have not helped so we undertook this project to see if they could be complementary. 相似文献12.
Ahmed S Abdel-Moneim Ahmad E Abdel-Ghany Salama AS Shany 《Journal of biomedical science》2010,17(1):25
Background
The highly pathogenic H5N1 is a major avian pathogen that crosses species barriers and seriously affects humans as well as some mammals. It mutates in an intensified manner and is considered a potential candidate for the possible next pandemic with all the catastrophic consequences. 相似文献13.
Boaz G. Oliveira Maria C. A. Lima Ivan R. Pitta Suely L. Galdino Marcelo Z. Hernandes 《Journal of molecular modeling》2010,16(1):119-127
A theoretical study is presented with the aim to investigate the molecular properties of intermolecular complexes formed by
the monomeric units of polyvinylpyrrolidone (PVP) or polyethyleneglycol (PEG) polymers and a set of four imidazolidine (hydantoine)
derivatives. The substitution of the carbonyl groups for thiocarbonyl in the hydantoin scaffold was taken into account when
analyzing the effect of the hydrogen bonds on imidazolidine derivatives. B3LYP/6-31G(d,p) calculations and topological integrations
derived from the quantum theory of atoms in molecules (QTAIM) were applied with the purpose of examining the N–H⋯O hydrogen
bond strengths formed between the amide group of the hydantoine ring and the oxygen atoms of PVP and PEG polymers. The effects
caused by the N–H⋯O interaction fit the typical evidence for hydrogen bonds, which includes a variation in the stretch frequencies
of the N–H bonds. These frequencies were identified as being vibrational red-shifts because their values decreased. Although
the values of such calculated interaction energies are between 12 and 33 kJ mol−1, secondary intermolecular interactions were also identified. One of these secondary interactions is formed through the interaction
of the benzyl hydrogen atoms with the oxygen atoms of the PVP and PEG structures. As such, we have analyzed the stretch frequencies
on the C–H bonds of the benzyl groups, and blue-shifts were identified on these bonds. In this sense, the intermolecular systems
formed by hydantoine derivatives and PVP/PEG monomers were characterized as a mix of red-shifting and blue-shifting hydrogen-bonded
complexes. 相似文献
14.
Giovane S. Galdino Steyner F. Cortes Igor D.G. Duarte Andrea C. Perez 《Life sciences》2010,86(13-14):505-509
AimsPhysical exercise is responsible for increasing the nociceptive threshold. The present study aimed to investigate the involvement of the nitric oxide/CGMP/KATP pathway in antinociception induced by acute aerobic exercise (AAc) in rats.Main methodsWistar rats performed exercise in a rodent treadmill, according to an AAc protocol. The nociceptive threshold was measured by mechanical and thermal nociceptive tests (paw-withdrawal, tail-flick and face-flick). To investigate the involvement of the NO/CGMP/KATP pathway the following nitric oxide synthase (NOS) unspecific and specific inhibitors were used: N-nitro-l-arginine (NOArg), Aminoguanidine, N5-(1-Iminoethyl)-l-ornithine dihydrocloride (L-NIO), Nω-Propyl-l-arginine (L-NPA); guanylyl cyclase inhibitor, 1H-[1,2,4]oxidiazolo[4,3-a]quinoxalin-1-one (ODQ); and KATP channel blocker, Glybenclamide; all administered subcutaneously at a dose of 2 mg/kg 10 min before exercise started. Plasma and cerebrospinal fluid (CSF) nitrite levels were determined by spectrophotometry.Key findingsIn the paw-withdrawal, tail-flick and face-flick tests, the AAc protocol produced antinociception, which lasted for more than 15 min. This effect was significantly reversed (P < 0.05) by NOS specific and unspecific inhibitors, guanylyl cyclase inhibitor (ODQ) and KATP channel blocker (Glybenclamide). Acute exercise was also responsible for increasing nitrite levels in both plasma and cerebrospinal fluid.SignificanceTaken together, these results suggest that the NO/CGMP/KATP pathway participates in antinociception induced by exercise. 相似文献
15.
Janaína A Couto Karina LA Saraiva Cleiton D Barros Daniel P Udrisar Christina A Peixoto Juliany SB César Vieira Maria C Lima Suely L Galdino Ivan R Pitta Maria I Wanderley 《Reproductive biology and endocrinology : RB&E》2010,8(1):13
Background
The present study was designed to examine the effect of chronic treatment with rosiglitazone - thiazolidinedione used in the treatment of type 2 diabetes mellitus for its insulin sensitizing effects - on the Leydig cell steroidogenic capacity and expression of the steroidogenic acute regulatory protein (StAR) and cholesterol side-chain cleavage enzyme (P450scc) in normal adult rats. 相似文献16.
Jessica AB van Nies Rute B Marques Stella Trompet Zuzana de Jong Fina AS Kurreeman Rene EM Toes J Wouter Jukema Tom WJ Huizinga Annette HM van der Helm-van Mil 《Arthritis research & therapy》2010,12(2):R38
Introduction
Recently an association between a genetic variation in TRAF1/C5 and mortality from sepsis or cancer was found in rheumatoid arthritis (RA). The most prevalent cause of death, cardiovascular disease, may have been missed in that study, since patients were enrolled at an advanced disease stage. Therefore, we used an inception cohort of RA patients to investigate the association between TRAF1/C5 and cardiovascular mortality, and replicate the findings on all-cause mortality. As TRAF1/C5 associated mortality may not be restricted to RA, we also studied a large cohort of non-RA patients. 相似文献17.
Guedes FL de Oliveira BG Hernandes MZ De Simone CA Veiga FJ de Lima Mdo C Pitta IR Galdino SL Neto PJ 《AAPS PharmSciTech》2011,12(1):401-410
Solid dispersions have been used as a strategy to improve the solubility, dissolution rate, and bioavailability of poor water-soluble
drugs. The increase of the dissolution rate presented by (5Z)-3-(4-chloro-benzyl)-5-(4-nitro-benzylidene)-imidazolidine-2,4-dione (LPSF/FZ4) from the solid dispersions is related to
the existence of intermolecular interactions of hydrogen bond type (>N–H...O<) between the amide group (>N–H) of the LPSF/FZ4 and the ether group (–O–) of the polyethyleneglycol polymer, or the carbonyl
(C=O) of the polyvinylpyrrolidone polymer (PVP). The intensity of these interactions is directly reflected in the morphology
acquired by LPSF/FZ4 in these systems, where a new solid phase, in the form of amorphous aggregates of irregular size, was
identified through scanning electron microscopy and confirmed in the characterizations achieved using X-ray diffraction and
thermal analysis of DSC. The solid dispersions with the polymer PVP, in higher concentrations, were revealed to be the best
option to be used in the formulations of LPSF/FZ4 in both theoretical and experimental studies. 相似文献
18.
19.
Cleiton Diniz Barros Angélica Amorim Amato Tiago Bento de Oliveira Karime Bicas Rocha Iannini Anekécia Lauro da Silva Teresinha Gonçalves da Silva Elisa Soares Leite Marcelo Zaldini Hernandes Maria do Carmo Alves de Lima Suely Lins Galdino Francisco de Assis Rocha Neves Ivan da Rocha Pitta 《Bioorganic & medicinal chemistry》2010,18(11):3805-3811
Eight new 5-arylidene-3-benzyl-thiazolidine-2,4-diones with halide groups on their benzyl rings were synthesized and assayed in vivo to investigate their anti-inflammatory activities. These compounds showed considerable biological efficacy when compared to rosiglitazone, a potent and well-known agonist of PPARγ, which was used as a reference drug. This suggests that the substituted 5-arylidene and 3-benzylidene groups play important roles in the anti-inflammatory properties of this class of compounds. Docking studies with these compounds indicated that they exhibit specific interactions with key residues located in the site of the PPARγ structure, which corroborates the hypothesis that these molecules are potential ligands of PPARγ. In addition, competition binding assays showed that four of these compounds bound directly to the ligand-binding domain of PPARγ, with reduced affinity when compared to rosiglitazone. An important trend was observed between the docking scores and the anti-inflammatory activities of this set of molecules. The analysis of the docking results, which takes into account the hydrophilic and hydrophobic interactions between the ligands and the target, explained why the 3-(2-bromo-benzyl)-5-(4-methanesulfonyl-benzylidene)-thiazolidine-2,4-dione compound had the best activity and the best docking score. Almost all of the stronger hydrophilic interactions occurred between the substituted 5-arylidene group of this compound and the residues of the binding site. 相似文献
20.
Pitta MG Silva AC Neves JK Silva PG Irmão JI Malagueño E Santana JV Lima MC Galdino SL Pitta IR Albuquerque MC 《Memórias do Instituto Oswaldo Cruz》2006,101(Z1):313-316
The emergence of strains of Schistosoma resistant to praziquantel has drawn attention to the search for new schistosomacide drugs. Imidazolidinic derivatives have performed outstandingly against adult S. mansoni worms when evaluated in vitro. The molecular modification of imidazolidine by way of bioisosteric replacement gives rise to variations in its biological response. This study verifies the potential of substituent groups in the derivatives (Z)3-benzyl-5-(2-fluoro-benzylidene)-imidazolidine-2,4-dione NE4, 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin -2-ona PT5, 3-benzyl-5-(3-fluoro-benzylidene)-1-methyl-2-thioxo-imidazolidin-4-one JT53; 3-benzyl-1-methyl-5-(4-methyl-benzylidene)-2-thioxo-imidazolidin-4-one JT63; 3-benzyl-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo -imidazolidin-4-one JT68; 3-(4-chloro-benzyl)-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo-imidazolidin-4-one JT69; 3-(4-phenyl-benzyl)-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo-imidazolidin-4-one JT72 by determining the viability in vitro of adult S. mansoni worms in the presence of these derivatives. The susceptibility of the worms obtained from mice and kept in culture in the presence of different concentrations was determined by way of schistosomacide kinetic, observed every 24 h over a period of eight days. The results show that the worms were more sensitive to the PT5 derivative at a concentration of 58 microM which killed 100% of the worms after 24 h of contact, also giving rise to alterations in the tegument surface of the worms with the formation of bubbles and peeling. These observations suggest a strong electronic contribution of the arylazo grouping in the biological response. 相似文献