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91.
M Dukat Y N Choi M Teitler A Du Pre K Herrick-Davis C Smith R A Glennon 《Bioorganic & medicinal chemistry letters》2001,11(12):1599-1603
The 5-HT(3) receptor binding affinities of nine pairs of aryl-substituted arylguanidines and arylbiguanides were examined and the results suggest the likelihood that both classes of agents utilize common receptor binding features. The effects of structural modification were also examined using CoMFA. 1-(3,4,5-Trichlorophenyl)guanidine (5-HT(3) K(i)=0.7 nM) was identified as a very high-affinity arylguanidine. The structures of the high-affinity arylguanidines are inconsistent with current 5-HT(3) pharmacophore models. 相似文献
92.
Prisinzano T Dukat M Law H Slassi A MacLean N DeLannoy I Glennon RA 《Bioorganic & medicinal chemistry letters》2004,14(18):4697-4699
2-(Anilino)imidazolines were identified as novel human 5-HT(1D) receptor ligands, but offered no particular advantage over previously reported 2-(benzyl)imidazolines. Pharmacokinetic and functional data were obtained for selected 2-(benzyl)imidazoline derivatives. 相似文献
93.
Glennon RA Grella B Tyacke RJ Lau A Westaway J Hudson AL 《Bioorganic & medicinal chemistry letters》2004,14(2):527-529
3,5,6,11-Tetrahydro-2H-imidazo[1',2':1,2]pyrido[3,4-b]indole (10) might be viewed as a fusion structure of two classes of I(2) imidazoline receptor ligands: 2-(2-benzofuranyl)-2-imidazolines and beta-carbolines. Its high affinity (K(i)=7.3 nM) provides insight to how the two classes of agents might bind relative to one another at I(2) receptors. 相似文献
94.
The variable clinical manifestations of cystic fibrosis (CF) suggest the influence of modifier genes. Genetic and environmental factors that determine whether an individual will develop associated complications are still being determined. It has been proposed that the gene for hemochromatosis, HFE, may be a modifier locus for CF disease phenotype. Recent research has suggested a relationship between mutations to the HFE gene and the development of meconium ileus (MI) and liver disease in CF. This study aims to expand our knowledge of the HFE mutations C282Y and H63D carrier rate in an Irish population of CF allele carriers. PCR restriction enzyme analysis was performed on blood samples from CF patients to identify the C282Y and H63D mutations. HFE status of CF allele carriers and CF patients (Delta F508) homozygotes with and without meconium ileus was determined. The carrier frequency for C282Y was 30.8% for the Delta F508 homozygote MI positive group, as compared to 12.5% for the non-Delta F508 MI positive group but did not reach statistical significance (p = 0.27). Interestingly, no Delta F508 homozygote patients were homozygous for the C282Y mutation. 相似文献
95.
Jeffers P Raposo S Lima-Costa ME Connolly P Glennon B Kieran PM 《Biotechnology letters》2003,25(23):2023-2028
Laser light scattering technology, as applied in the Lasentec focussed beam reflectance measurement (FBRM) system, was used to characterise two morphologically dissimilar plant cell suspension cultures, Morinda citrifolia and Centaurea calcitrapa. Shake-flask suspensions were analysed in terms of biomass concentration and aggregate size/shape over the course of typical batch growth cycles. For the heavily aggregated C. calcitrapa, biomass levels [from 10-160 g fresh weight (fw) l(-1))] were linearly correlated with FBRM counts. For M. citrifolia, which grows in unbranched chains of 2-10 elongated cells, linear correlation of biomass concentration with FBRM counts was applicable in the range 0-100 g fw l(-1); at higher levels (100-300 g fw l(-1)), biomass was non-linearly correlated with FBRM counts and length-weighted average FBRM chord length. For both cell systems, particle morphology (size/shape) was quantified using semi-automated digital image analysis. The average aggregate equivalent diameter (C. calcitrapa) and average chain length (M. citrifolia), determined using image analysis, closely tracked the FBRM average chord length. The data clearly demonstrate the potential for applying the FBRM technique for rapid characterisation of plant cell suspension cultures. 相似文献
96.
Characterization of 3-chlorobenzoate degrading aerobic bacteria isolated under various environmental conditions 总被引:2,自引:0,他引:2
Krooneman J Sliekers AO Pedro Gomes TM Forney LJ Gottschal JC 《FEMS microbiology ecology》2000,32(1):53-59
The rates of bacterial growth in nature are often restricted by low concentrations of oxygen or carbon substrates. In the present study the metabolic properties of 24 isolates that had been isolated using various concentrations of 3-chlorobenzoate, benzoate and oxygen as well as using continuous culture at high and low growth rates were determined to investigate the effects of these parameters on the metabolism of monoaromatic compounds. Bacteria were enriched from different sampling sites and subsequently isolated. In batch culture this was done both under low oxygen (2% O(2)) and air-saturated concentrations. Chemostat enrichments were performed under either oxygen or 3-chlorobenzoate limiting conditions. Bacteria metabolizing aromatics with gentisate or protocatechuate as intermediates (gp bacteria) as well as bacteria metabolizing aromatic compounds via catechols (cat bacteria) were isolated from batch cultures when either benzoate or 3CBA were used as C sources, regardless of the enrichment conditions applied. In contrast, enrichments performed in chemostats at low dilution rates resulted in gp-type organisms only, whereas at high dilution rates cat-type organisms were enriched, irrespective of the oxygen and 3-chlorobenzoate concentration used during enrichment. It is noteworthy that the gp-type of bacteria possessed relatively low μ(max) values on 3CBA and benzoate along with relatively high substrate and oxygen affinities for these compounds. This is in contrast with cat-type of bacteria, which seemed to be characterized by high maximum specific growth rates on the aromatic substrates and relatively high apparent half saturation constants. In contrast, bacteria degrading chlorobenzoate via gentisate or protocatechuate may possibly be better adapted to conditions leading to growth at reduced rates such as low oxygen and low substrate concentrations. 相似文献
97.
Belinda Kahnt Wesley N. Hattingh Panagiotis Theodorou Nicolas Wieseke Michael Kuhlmann Kelsey L. Glennon Timotheüs van der Niet Robert Paxton Glynis V. Cron 《Molecular ecology》2019,28(17):4118-4133
Plant–pollinator interactions are often highly specialised, which may be a consequence of co‐evolution. Yet when plants and pollinators co‐evolve, it is not clear if this will also result in frequent cospeciation. Here, we investigate the mutual evolutionary history of South African oil‐collecting Rediviva bees and their Diascia host plants, in which the elongated forelegs of female Rediviva have been suggested to coevolve with the oil‐producing spurs of their Diascia hosts. After controlling for phylogenetic nonindependence, we found Rediviva foreleg length to be significantly correlated with Diascia spur length, suggestive of co‐evolution. However, as trait correlation could also be due to pollinator shifts, we tested if cospeciation or pollinator shifts have dominated the evolution of Rediviva–Diascia interactions by analysing phylogenies in a cophylogenetic framework. Distance‐based cophylogenetic analyses (PARAFIT, PACo) indicated significant congruence of the two phylogenies under most conditions. Yet, we found that phylogenetic relatedness was correlated with ecological similarity (the spectrum of partners that each taxon interacted with) only for Diascia but not for Rediviva, suggesting that phylogenetic congruence might be due to phylogenetic tracking by Diascia of Rediviva rather than strict (reciprocal) co‐evolution. Furthermore, event‐based reconciliation using a parsimony approach (CORE‐PA) on average revealed only 11–13 cospeciation events but 58–80 pollinator shifts. Probabilistic cophylogenetic analyses (COALA) supported this trend (8–29 cospeciations vs. 40 pollinator shifts). Our study suggests that diversification of Diascia has been largely driven by Rediviva (phylogenetic tracking, pollinator shifts) but not vice versa. Moreover, our data suggest that, even in co‐evolving mutualisms, cospeciation events might occur only infrequently. 相似文献
98.
RG Lockie AB Schultz SJ Callaghan CA Jordan TM Luczo MD Jeffriess 《Biology of sport / Institute of Sport》2015,32(1):41-51
There is little research investigating relationships between the Functional Movement Screen (FMS) and athletic performance in female athletes. This study analyzed the relationships between FMS (deep squat; hurdle step [HS]; in-line lunge [ILL]; shoulder mobility; active straight-leg raise [ASLR]; trunk stability push-up; rotary stability) scores, and performance tests (bilateral and unilateral sit-and-reach [flexibility]; 20-m sprint [linear speed]; 505 with turns from each leg; modified T-test with movement to left and right [change-of-direction speed]; bilateral and unilateral vertical and standing broad jumps; lateral jumps [leg power]). Nine healthy female recreational team sport athletes (age = 22.67 ± 5.12 years; height = 1.66 ± 0.05 m; body mass = 64.22 ± 4.44 kilograms) were screened in the FMS and completed the afore-mentioned tests. Percentage between-leg differences in unilateral sit-and-reach, 505 turns and the jumps, and difference between the T-test conditions, were also calculated. Spearman''s correlations (p ≤ 0.05) examined relationships between the FMS and performance tests. Stepwise multiple regressions (p ≤ 0.05) were conducted for the performance tests to determine FMS predictors. Unilateral sit-and-reach positive correlated with the left-leg ASLR (r = 0.704-0.725). However, higher-scoring HS, ILL, and ASLR related to poorer 505 and T-test performance (r = 0.722-0.829). A higher-scored left-leg ASLR related to a poorer unilateral vertical and standing broad jump, which were the only significant relationships for jump performance. Predictive data tended to confirm the correlations. The results suggest limitations in using the FMS to identify movement deficiencies that could negatively impact athletic performance in female team sport athletes. 相似文献
99.
Kim JS Padnya A Weltzin M Edmonds BW Schulte MK Glennon RA 《Bioorganic & medicinal chemistry letters》2007,17(17):4855-4860
Desformylflustrabromine (dFBr; 1) and desformylflustrabromine-B (dFBr-B; 2) have been previously isolated from natural sources, and the former has been demonstrated to be a novel and selective positive allosteric modulator of alpha4beta2 nicotinic acetylcholine (nACh) receptors. The present study describes the synthesis of water-soluble salts of 1 and 2, and confirms and further investigates the actions of 1 and 2 using two-electrode voltage clamp recordings. 相似文献
100.
Abstract Anhydro 1- (2', 3', 5’ -tri-Oacetyl-β-D-ribofuranosyl) -5-hydroxy-7-oxoimidazo[2, 1-b]-1, 3-thiazinium hydroxide, a mesoionic imidazothiazine nucleoside, was prepared by the condensation of the appropriately acetylated ribofuranosyl imidazoline-2-thione with carbon suboxide. Although stable at or below O° C, the product rapidly underwent ring-opening at room temperature to afford the precursor nucleoside. A possible scheme for this ring-opening reaction is proposed based on the results of a model study employing anhydro 1-methyl-5-hydrcxy-7-oxoimidazo[2, 1-b]-1, 3-thiazinium hydroxide. 相似文献