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1.
The Texas coastline stretches 595 km across almost 4° of latitude and is home to diverse coastal vegetation assemblages, yet only a handful of studies have documented the climate and vegetative change of this region through the Holocene. We provide a detailed palynological record of Holocene climate for coastal Texas, based upon three subaqueous sediment cores from Corpus Christi Bay and Trinity Bay. Cluster analysis and correspondence analysis were used to investigate changes in palynological assemblages through time within each core. Common to both bays are nonarboreal taxa including Asteraceae (mainly Ambrosia and Helianthus), Chenopodium, Poaceae, and arboreal taxa such as Carya, Pinus, and Quercus. Our record shows that the coastal environments of central Texas began a transition from herbaceous (nonarboreal) dominated vegetation to arboreal vegetation as early as 8.4 ka within Corpus Christi Bay, and 3.8 ka within Trinity Bay. We note flooding events at 8.2, 5.4, and 3.6 ka in Corpus Christi Bay, and at 1.7, 1.2, and 0.8 ka in Trinity Bay. These events were caused by storms, sea level changes including flooding of relict river terraces, and changes in sediment delivery to the bays. The pollen record also shows evidence for changes in fluvial discharge to Corpus Christi Bay at 4.1 and 2.2 ka, and at 1.8 ka in Trinity Bay. We also see Zea mays in Trinity Bay, indicating local Native American agriculture. We observe no significant changes during the middle Holocene Climatic Optimum, and subtle but not statistically significant evidence of more variable climate oscillations than other records from more interior sites in Texas available for the late Holocene. This indicates that coastal Texas’ climate has operated semi-independently from central Texas regions, and was primarily driven by a coast-wise gradient of precipitation and evapotranspiration.  相似文献   

2.
The shell length, height, and width, live body weight, and edible tissue weight of Manila clam of 1, 2, and 3 years of age were measured, and their correlation coefficients were calculated. The shell morphological traits were used as independent variables, and live body weight or edible tissue weigh used as a dependent variable for calculating the path coefficients, correlation index and determination coefficients. The results showed that the correlation coefficients between each shell morphological trait and the live body weight or edible tissue weight were all highly significant (P < 0. 01). The shell height at 1-year old clams was highly correlated with the live body weight and edible tissue weight. The shell width of 2- to 3-year-old clams was strongly associated with the live body weight, while the shell length was closely linked to the edible tissue weight. The results of coefficients of determination for the morphological traits against weight traits agreed well with the results of path analysis. The correlation indices for all morphological traits against weight traits were approximately the same as determination coefficients regardless of clam age. The correlation indices (R2) of morphological traits against the live body weight of clams of all ages and edible tissue weight of 1-year-old clams were larger than 0.85, but R2 of morphological traits against the edible tissue weight of 2- and 3-year-old clams was smaller than 0.85, indicating that some other factors might be associated with the edible tissue weight of 2- and 3-year-old clams. Multiple regression equations were obtained to estimate shell length X1 (cm), shell height X2 (cm), shell width X3 (cm) against live body weight Y (g), edible tissue weight Z (g): for 1-year-old clams: Y = ?4.317 + 0.18X1 + 0.147X2, (X1 < 0.01, X2 < 0.01), Z = ?1.011 + 0.095X2, (X2 < 0.01); for 2-year-old clams: Y = ?15.119 + 0.249X1 + 0.176X2 + 0.688X3, (X1 < 0.01, X3 < 0.01), Z = ?4.248 + 0.198X1, (X1 < 0.05, X3 < 0.01); and for 3-year-old clams: Y = ?25.013 + 0.415X1 + 1.184X3, (X1 < 0.01, X3 < 0.01), Z = ?7.082 + 0.119X1 + 0.332X3, (X1 < 0.05, X3 < 0.01).  相似文献   

3.
Water transparency is one of the ecological indicators for describing water quality and the underwater light field which determines its productivity. In the European Water Framework Directive (WFD) as well as in the European Marine Strategy Framework Directive (MSFD) water transparency is used for ecological status classification of inland, coastal and open sea waters and it is regarded as an indicator for eutrophication in Baltic Sea management (HELCOM, 2007). We developed and compared different empirical and semi-analytical algorithms for lakes and coastal Nordic waters to retrieve Secchi depth (ZSD) from remote sensing data (MERIS, 300 m resolution). The algorithms were developed in water bodies with high coloured dissolved organic matter absorption (aCDOM(442) ranging 1.7–4.0 m−1), Chl a concentration (0.5–73 mg m−3) and total suspended matter (0.7–37.5 g m−3) and validated against an independent data set over inland and coastal waters (0.6 m < ZSD < 14.8 m). The results indicate that for empirical algorithms, using longer wavelengths in the visible spectrum as a reference band decreases the RMSE and increases the coefficient of determination (R2). The accuracy increased (R2 = 0.75, RMSE = 1.33 m, n = 134) when ZSD was retrieved via an empirical relationship between ZSD and Kd(490). The best agreement with in situ data was attained when ZSD was calculated via both the diffuse and the beam attenuation coefficient (R2 = 0.89, RMSE = 0.77 m, n = 89). The results demonstrate that transparency can be retrieved with high accuracy over various optical water types by the means of ocean color remote sensing, improving both the spatial and temporal coverage. The satellite derived ZSD product could be therefore used as an additional source of information for WFD and MSFD reporting purposes.  相似文献   

4.
Flooding periods can be one of the most important factors influencing nitrogen (N) biogeochemical processes in wetlands ecosystem. We conducted a field study using in situ incubation method to investigate the seasonal dynamics of soil net N mineralization in three coastal salt marshes (Suaeda salsa) with different flooding periods (i.e., short-term (STF), seasonal (SF), and tidal (TF) flooding wetland) in the Yellow River Delta. Selected soil inorganic N pools (ammonium, nitrate and inorganic N) and N transformation (mineralization, nitrification and ammonification) rates in the top 0–10 cm soils were repeatedly quantified from April to October. Clear seasonal patterns in inorganic N pools and transformation rates were observed in accord with the seasonal variations of temperature and moisture. Generally, higher levels of soil inorganic nitrogen, ammonium nitrogen (NH4+-N) and nitrate nitrogen (NO3-N) occurred in the early-growing season (April), and NH4+-N contents got a small accumulative peak in midsummer (September). The lower rates (negative) of net mineralization (Rmin), nitrification (Rnit) and ammonification (Ramm) were observed in the early-growing season (April–June) and fall (September–October), whereas higher values (positive) in midsummer (August–September). Flooding had a significant influence on inorganic N pools (except for NH4+-N) and transformation rates (p < 0.05). Rmin values in SF wetland were significantly higher in the August-September period than those in other incubation periods. Rnit values in TF wetland exhibited a small variation and the highest value occured in the June–August period. The results of principal component analysis showed that soil samples were clearly divided into two groups before and after flow-sediment regulation. After flooding events, the Rmin and Ramm values generally increased in the three wetlands, whereas a significant decrease in Rnit values was observed in SF wetland (p < 0.05), thus the differences in NO3-N among these wetlands were eliminated. These results suggested that seasonal variations in temperature and moisture are important factors influencing inorganic N pools and transformation rates.  相似文献   

5.
A group of N-1 and C-3 disubstituted-indole Schiff bases bearing an indole N-1 (R′ = H, CH2Ph, COPh) substituent in conjunction with a C-3 –CHN–C6H4–4-X (X = F, Me, CF3, Cl) substituent were synthesized and evaluated as inhibitors of cyclooxygenase (COX) isozymes (COX-1/COX-2). Within this group of Schiff bases, compounds 15 (R1 = CH2Ph, X = F), 17 (R1 = CH2Ph, X = CF3), 18 (R1 = COPh, X = F) and 20 (R1 = COPh, X = CF3) were identified as effective and selective COX-2 inhibitors (COX-2 IC50’s = 0.32–0.84 μM range; COX-2 selectivity index (SI) = 113 to >312 range). 1-Benzoyl-3-[(4-trifluoromethylphenylimino)methyl]indole (20) emerged as the most potent (COX-1 IC50 >100 μM; COX-2 IC50 = 0.32 μM) and selective (SI >312) COX-2 inhibitor. Furthermore, compound 20 is a selective COX-2 inhibitor in contrast to the reference drug indomethacin that is a potent and selective COX-1 inhibitor (COX-1 IC50 = 0.13 μM; COX-2 IC50 = 6.9 μM, COX-2 SI = 0.02). Molecular modeling studies employing compound 20 showed that the phenyl CF3 substituent attached to the CN spacer is positioned near the secondary pocket of the COX-2 active site, the CN nitrogen atom is hydrogen bonded (N?NH = 2.85 Å) to the H90 residue, and the indole N-1 benzoyl is positioned in a hydrophobic pocket of the COX-2 active site near W387.  相似文献   

6.
A new strain of Manila clam with orange shell color was produced after selection within a full-sib family for two generations. In the present study, the shell length, height, and width, and the live body weight of the orange strain were measured, and their correlation coefficients were calculated. The shell morphological traits were used as independent variables, and the live body weight was used as the dependent variable for calculating the path coefficients, correlation index, and determination coefficients. The results showed that the correlation coefficients between each shell morphological trait and the live body weight were all highly significant (P < 0.01). The correlation indices (R2) of morphological traits against the live body weight of clams were larger than 0.85, indicating that the morphology traits were the main factors affecting the body weight. Multiple regression equations were obtained to estimate shell length X1 (cm), shell height X2 (cm), and shell width X3 (cm) against live body weight Y (g): Y = ? 2.62 + 0.34 X1 + 0.145 X2, (X1 < 0.05, X2 < 0.05). The results suggest that the shell length could be used as the main trait for selective breeding and could indirectly make a large improvement in the weight trait.  相似文献   

7.
Composition and phase dependence of the mixing of 1,2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), and 1,2-Dioleoyl-sn-glycero-3-phosphocholine (DOPC), with the oxidized phospholipid, 1-palmitoyl-2-glutaryl-sn-glycero-3-phosphocholine (PGPC) were investigated by characterizing the aggregation states of DPPC/PGPC and DOPC/PGPC using a fluorescence quenching assay, dynamic light scattering, and time-resolved fluorescence quenching in the temperature range 5–60 °C. PGPC forms 3.5 nm radii micelles of aggregation number 33. In the gel phase, DPPC and PGPC fuse to form mixed vesicles for PGPC molar fraction, XPGPC  0.3 and coexisting vesicles and micelles at higher XPGPC. Data suggest that liquid phase DPPC at 50 °C forms mixed vesicles with segregated or hemi fused DPPC and PGPC for XPGPC  0.3. At 60 °C, DPPC and PGPC do not mix, but form coexisting vesicles and micelles. DOPC and PGPC do not mix in any proportion in the liquid phase. Two dissimilar aggregates of the sizes of vesicles and PGPC micelles were observed for all XPGPC for T  22 °C. DOPC–PGPC and DPPC–PGPC mixing is non-ideal for XPGPC > 0.3 in both gel and fluid phases resulting in exclusion of PGPC from the bilayer. Formation of mixed vesicles is favored in the gel phase but not in the liquid phase for XPGPC  0.3. For XPGPC  0.3, aggregation states change progressively from mixed vesicles in the gel phase to component segregated mixed vesicles in the liquid phase close to the chain melting transition temperature to separated coexisting vesicles and micelles at higher temperatures.  相似文献   

8.
Little information is available to assess the dynamic changes in wetland soil quality in coastal regions, though it is essential for wetland conservation and management. Soil samples were collected in Suaeda salsa wetlands (SWs), Tamarix chinensis wetlands (TWs), Suaeda salsaTamarix chinensis wetlands (STWs), freshwater Phragmites australis wetlands (FPWs) and saltwater Phragmites australis wetlands (SPWs) in three sampling periods (i.e., summer and autumn of 2007 and spring of 2008). According to the flooding characteristics of these wetlands, the study area could be grouped into three sub-regions: short-term flooding region (STFR), seasonal flooding region (SFR) and tidal flooding region (TFR). Soil quality was evaluated using the soil quality index (SQI), which was calculated using the selected minimum data set (MDS) based on principal components analysis (PCA). Our results showed that soil salt content (SSC), total carbon (TC), magnesium (Mg), nitrate nitrogen (NO3-N) and total sulfur (TS) consisted of a MDS among 13 soil properties. The SQI values varied from 0.18 to 0.66 for all soil samples, of which the highest and lowest SQI values were observed in TFR. The average SQI values were significantly higher in summer (0.50 ± 0.13) than in spring (0.37 ± 0.13) and autumn (0.36 ± 0.11) in the whole study area (p < 0.05). The average SQI values followed the order STFR (0.44 ± 0.12) > TFR (0.41 ± 0.15) > SFR (0.35 ± 0.09) although no significant differences were observed among the three regions (p > 0.05). SPWs and SWs soils showed higher SQI values (0.50 ± 0.10 and 0.47 ± 0.15, respectively) than TWs (0.30 ± 0.08) soils (p < 0.05). The SSC was the dominant factor of soil quality with its proportion of 34.1% contributing to the SQI values, followed by TC (24.5%) and Mg (24.1%). Correlation analysis also showed that SQI values were significantly negatively correlated with SSC. SSC might be a characteristic indicator of wetland soil quality assessment in coastal regions. The findings of this study showed that the SQI based on MDS is a powerful tool for wetland soil quality assessment.  相似文献   

9.
This study mainly focused on the modification of the X2 position in febuxostat analogs. A series of 1-phenyl-1H-1,2,3-triazole-4-carboxylic acid derivatives (1a-s) with an N atom occupying the X2 position was designed and synthesized. Evaluation of their inhibitory potency in vitro on xanthine oxidase indicated that these compounds exhibited micromolar level potencies, with IC50 values ranging from 0.21 µM to 26.13 μM. Among them, compound 1s (IC50 = 0.21 μM) showed the most promising inhibitory effects and was 36-fold more potent than allopurinol, but was still 13-fold less potent than the lead compound Y-700, which meant that a polar atom fused at the X2 position could be unfavorable for potency. The Lineweaver-Burk plot revealed that compound 1s acted as a mixed-type xanthine oxidase inhibitor. Analysis of the structure-activity relationships demonstrated that a more lipophilic ether tail (e.g., meta-methoxybenzoxy) at the 4′-position could benefit the inhibitory potency. Molecular modeling provided a reasonable explanation for the structure–activity relationships observed in this study.  相似文献   

10.
The introduced shrub Tamarix ramosissima invades riparian zones, but loses competitiveness under flooding. Metabolic effects of flooding could be important for T. ramosissima, but have not been previously investigated. Photosynthesis rates, stomatal conductance, internal (intercellular) CO2, transpiration, and root alcohol dehydrogenase (ADH) activity were compared in T. ramosissima across soil types and under drained and flooded conditions in a greenhouse. Photosynthesis at 1500 μmol quanta m−2 s−1 (A1500) in flooded plants ranged from 2.3 to 6.2 μmol CO2 m−2 s−1 during the first week, but A1500 increased to 6.4–12.7 μmol CO2 m−2 s−1 by the third week of flooding. Stomatal conductance (gs) at 1500 μmol quanta m−2 s−1 also decreased initially during flooding, where gs was 0.018 to 0.099 mol H2O m−2 s−1 during the first week, but gs increased to 0.113–0.248 mol H2O m−2 s−1 by the third week of flooding. However, photosynthesis in flooded plants was reduced by non-stomatal limitations, and subsequent increases indicate metabolic acclimation to flooding. Root ADH activities were higher in flooded plants compared to drained plants, indicating oxygen stress. Lower photosynthesis and greater oxygen stress could account for the susceptibility of T. ramosissima at the onset of flooding. Soil type had no effect on photosynthesis or on root ADH activity. In the field, stomatal conductance, leaf water potential, transpiration, and leaf δ13C were compared between T. ramosissima and other flooded species. T. ramosissima had lower stomatal conductance and water potential compared to Populus deltoides and Phragmites australis. Differences in physiological responses for T. ramosissima could become important for ecological concerns.  相似文献   

11.
Screening of a 65,536-member one-bead-one-compound (OBOC) combinatorial library of glycopeptide dendrimers of structure ((βGal)n + 1X8X7X6X5)2DapX4X3X2X1(β-Gal)m (βGal = β-galactosyl-thiopropionic acid, X8–1 = variable amino acids, Dap = l-2,3-diaminopropionic acid, n, m = 0, or 1 if X8 = Lys resp. X1 = Lys) for binding of Jurkat cells to the library beads in cell culture, resynthesis and testing lead to the identification of dendrimer J1 (βGal-Gly-Arg-His-Ala)2Dap-Thr-Arg-His-Asp-CysNH2 and related analogues as delivery vehicles. Cell targeting is evidenced by FACS with fluorescein conjugates such as J1F. The colchicine conjugate J1C is cytotoxic with LD50 = 1.5 μM. The β-galactoside groups are necessary for activity, as evidenced by the absence of cell-binding and cytotoxicity in the non-galactosylated, acetylated analogue AcJ1F and AcJ1C, respectively. The pentagalactosylated dendrimer J4 βGal4(Lys-Arg-His-Leu)2Dap-Thr-Tyr-His-Lys(βGal)-Cys) selectively labels Jurkat cell as the fluorescein derivative J4F, but its colchicine conjugate J4C lacks cytotoxicity. Tubulin binding assays show that the colchicine dendrimer conjugates do not bind to tubulin, implying intracellular degradation of the dendrimers releasing the active drug.
  相似文献   

12.
Population size of migratory birds responds to various types of environmental factors, which affect different stages of bird population. In the current study, we analyzed a long-term avifauna monitoring database to investigate population changes in the migratory bird Little Tern, Sternula albifrons, with respect to a quasi-natural disturbance, flooding, induced by a regional characteristic climate pattern, the Korean Monsoon (KM), in the Nakdong River Estuary of South Korea. We scrutinized the time-delayed influence by means of wavelet transformation and year-to-year comparison. Little Tern individuals started to grow in April, and reached its maximum generally in May or June, and an abrupt decrease of individual number was observed after KM occurred. Sequential time-series analysis based on wavelet transformation revealed that the changing pattern of the population size of Little Tern in the estuary was linked to the previous year's flooding (a 9- to 10-month delay), which is regarded as the time difference between Little Tern breeding season and previous KM period. Stronger flooding waters during KM season expelled comparably more individuals of Little Tern from the estuary (r2 = 0.595; p < 0.05; n = 9), and the more the individuals left, the smaller the bird arrived at the estuary in the next year. Further examination revealed that earlier initiation and longer duration of KM in yeart  1 negatively affected the newly arriving Little Tern individuals in the current year (i.e., yeart; r2 = 0.809 for impact of KM onset, r2 = 0.909 for impact of KM duration; n = 10, respectively; p < 0.005). The Little Tern population gradually increased when summer flooding was not strong in the previous successive years, from which we concluded that the population of the migratory bird Little Tern tends to adapt to quasi-natural disturbance (flooding) to maintain their population size.  相似文献   

13.
Due to the similarity between Pd and Pt, the complexes of palladium(II) can be considered as potential anticancer agents. Activity of six PdCl2(X2Py)2 complexes (Py = pyridine, and X = CH3 or Cl) was measured by MTT test using MCF7, CCRF-SB, PC3 and human B-lymphoblastoid cell lines. We found that the effect of PdCl2(XnPy)2 was cell-specific and time-dependent. Obtained results were discussed and compared with the activation parameters calculated for the hydrolysis of PdCl2(XnPy)2, indicating a correlation between viability of MCF7 and CCRF-SB cells and rates of hydrolysis of the Pd(II) complexes.  相似文献   

14.
Thirty two morphologically different bacterial were isolated from different soil samples and screened for their ability to produce lipolytic enzymes. Among all isolates, the isolate coded AZ1 was selected due to its high potency to produce lipase at elevated temperature up to 65 °C. Phylogenetic analysis based on 16SrDNA sequence revealed its close relationship to Geobacillus thermodenitrificans. The effect of ten culture variable on lipase production was evaluated by implementing Plackett–Burman statistical design. d-sucrose, peptone and soy bean flour were the most significant variables affecting lipase production. A pre-optimized medium based on this experiment yielded an enzyme activity of 260 U min?1 ml?1. For further optimization, a fourteen trials’ multi-factorial Box–Behnken experimental design was applied to find out the optimum level of each of the significant variables. The tested variables, namely: d-sucrose (X1); peptone (X2) and soy bean flour (X3) were examined, each at three different levels coded ?1, 0, +1. The optimal levels of the three components were founded to be (g/L): d-sucrose, 6.56; peptone, 6.35; and soy bean flour, 6.92, with a predicted activity of approximately 610 U min?1 ml?1. According to the results of the Plackett–Burman and Box–Behnken designs the following medium composition is expected to be optimum (g/L): d-sucrose 6.56, peptone 6.35, soy bean flour 6.92, CaCl2 0.02, Y.E. 2.5, K2HPO4 1.0, MgSO4.7H2O 0.2 and Fe2 (SO4)3 0.02; pH, 8; cultivation temperature 55 °C and incubation time 24 h, the enzyme activity measured in the medium was approximately 593 U min?1 ml?1.  相似文献   

15.
The success of interpolation techniques relies heavily on the density and regularity of field reference data points. For instance temperature interpolations in the Arctic are hampered by few and scattered meteorological stations. The major objective of this study is to analyze the spatial relationship between plants, defined in terms of an index of thermophily (It) and temperature distribution. The study area is located in Kongsfjorden, northwest Spitsbergen (Svalbard). A systematic recording of floristic data covering the study area was made within quadrates of 1 km × 1 km (93 units). For each of them, the It was calculated. It provides a synthetic measure by which plants are taken as temperature indicators at a long time scale. Temperature values were recorded by means of 39 temperature loggers during the summer 2000. The model for spatial interpolation of temperature was developed using multiple regression of remote sensed data (Landsat TM) and topographical features derived from a digital elevation model (DEM). Continuous temperature layers were calculated at a spatial resolution of 50 m × 50 m, and aggregated to a resolution of 1 km × 1 km in order to correspond with the observed botanical units. Different maps were produced showing spatial distribution of the modelled temperature and It. Correlations between the It and temperature values derived from the modelled temperature layers were systematically explored. Correlation between the It and temperatures works well as standard deviation of residues is 0.7 °C only. Highest correlations (r) of It and the spatial distribution of temperature were obtained for: (a) maximum average temperature for August, excluding all areas higher than 100 m above sea level (0.75), (b) average daily maximum temperature for July–October (0.67), (c) average temperature for July and August (0.64, 0.65), and (d) when temperature range is >8 °C (0.55). Areas with low correlations between It and temperature were mainly attributed to the fact that these measurements represent (a) different time scales and (b) different spatial scales. However, results from this study have shown that calculating It provide a mean for restoring selected temperature parameters and thus can contribute to fill in and extend the network of field data points for temperature interpolation purposes.  相似文献   

16.
《Mammalian Biology》2014,79(6):384-392
The South American sea lion (Otaria byronia) (SSL) is a widespread opportunistic predator that inhabits waters ranging from Southern Ecuador to Southern Chile in the Pacific Ocean and from Southern Brazil to Southern Argentina in the Atlantic. SSL abundance estimates, as for many pinniped species, have relied on shore censuses, with the uncertainty that an indeterminate number of individuals at sea might remain uncounted. The proportion of the population that remains at sea during censuses and their distribution patterns are not clear and has been scarcely assessed. We used line transect sampling to gather information about at-sea abundance, density and spatial distribution of SSL in coastal waters off the Chilean Northern Patagonia. A total of 123 groups were sighted while on-effort, with an estimated density of 0.393 ind./km2 (95%CI = 0.262–0.591) and a total abundance, for the surveyed area, of 13,721 individuals (95%CI = 9127–20,627). Even when our survey was rather restricted in spatial range, generalized additive model results showed that depth, distance to SSL rockeries, coastline complexity and geographical coordinates had a significant influence on SSL spatial distribution. The results on abundance and spatial distribution of SSL at sea are discussed in terms of current population estimates. Our substantial at-sea abundance estimate suggests that shore censuses might have been historically biased. Several aspects should be taken into account in further research on SSL abundance, such as including pelagic waters and undertaking simultaneously on-rockery and marine SSL abundance estimates. The results presented here provide valuable insights for revisiting and possibly improve population estimates of SSL and other pinnipeds species worldwide. This is particularly relevant when management and conservation actions need to be taken on those species that have strong interactions with fisheries and aquaculture.  相似文献   

17.
《Inorganica chimica acta》2006,359(5):1613-1618
Two trinuclear Pd(II) nitrosyl carboxylate complexes Pd3(NO)2(μ-OCOCX3)42-ArH)2 (X = F, ArH = toluene, 3a; X = Cl, ArH = benzene, 3b) have been prepared and structurally characterized. These display a linear Pd3 array capped by terminal bent NO ligands and η2-coordinated molecules of aromatic molecules. Solution IR and NMR measurements indicate that the solid state structure of 3a is partially maintained in solution, while 3b loses benzene when dissolved in dichloromethane.  相似文献   

18.
A novel series of prodrugs containing dabigatran and methyl (E)-3-(4-hydroxy-2-methoxyphenyl)propenoate (methyl ferulate) were synthesized. All of them reveal the effect of thrombin-induced anti-platelet aggregation in vitro. In addition, in vivo experiment shows that one of the target compounds, X-2 (ED50 = 3.7 ± 1.0 μmol/kg) possesses a more potent activity for inhibiting venous thrombosis than that of dabigatran etexilate (ED50 = 7.8 ± 1.5 μmol/kg).  相似文献   

19.
《Inorganica chimica acta》2006,359(5):1643-1649
Spontaneous resolution in solvothermal reactions through tuning the volume of the templating and space-filling agents (quaternary ammonium cations) lead to three novel halogeno(cyano)cuprates [R4N][Cu(CN)X] (R = Et, X = Cl, 1; R = Et, X = Br, 2; R = Bu, X = I, 3), which all consist of 1-D helical chains. Compounds 1 and 2 reveal to be mesomeric structures while compound 3 exhibits a nonracemic enantiopure topology. Luminescent studies indicate that all three compounds are potential materials for efficient luminescent materials.  相似文献   

20.
Chagas disease (American trypanosomiasis) is one of the most important parasitic diseases with serious social and economic impacts mainly on Latin America. This work reports the synthesis, in vitro trypanocidal evaluation, cytotoxicity assays, and molecular modeling and SAR/QSAR studies of a new series of N-phenylpyrazole benzylidene-carbohydrazides. The results pointed 6k (X = H, Y = p-NO2, pIC50 = 4.55 M) and 6l (X = F, Y = p-CN, pIC50 = 4.27 M) as the most potent derivatives compared to crystal violet (pIC50 = 3.77 M). The halogen-benzylidene-carbohydrazide presented the lowest potency whereas 6l showed the most promising profile with low toxicity (0% of cell death). The best equation from the 4D-QSAR analysis (Model 1) was able to explain 85% of the activity variability. The QSAR graphical representation revealed that bulky X-substituents decreased the potency whereas hydrophobic and hydrogen bond acceptor Y-substituents increased it.  相似文献   

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