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1.
PeerJ ; 8: e8615, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32117637

RESUMO

This study evaluates the applicability of the Tropical Rain Measurement Mission (TRMM) 3B43V7 product for use throughout mainland China. Four statistical metrics were used based on the observations made by rain gauges; these metrics were the correlation coefficient (R), the relative bias (RB), the root mean square error (RMSE) and Nash-Sutcliffe efficiency (NSE), and they were chosen to evaluate the performance of the 3B43V7 product at temporal and spatial scales. The results revealed that 3B43V7 performed satisfactorily on all timescales (R > 0.9 and NSE > 0.86); however, it overestimated the results when compared with the rain gauge observations in certain circumstances (RB = 9.7%). Monthly estimates from 3B43V7 were in agreement with rain gauge observations. 3B43V7 can effectively capture the seasonal patterns of precipitation characteristics over mainland China. However, 3B43V7 tends to register a greater overestimation of precipitation in the winter (RB = 14%) than in other seasons while showing greater consistency with the observations made by rain gauges during dry periods. The 3B43V7 product performs well in the eastern part of mainland China, while its performance is poor in the western part of mainland China. In terms of altitude, 3B43V7 performs satisfactorily in areas with moderate to low altitudes (when altitude < 3,500 m, R > 0.9, NSE > 0.8 and RB < 10.2%) but RB values increase with altitude. Overall, 3B43V7 had a favorable performance throughout mainland China.

2.
Sensors (Basel) ; 20(3)2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-32050517

RESUMO

The Huang-Huai-Hai (3H) Plain is the major crop-producing region in China. Due to the long-term overexploitation of groundwater for irrigation, the groundwater funnel is constantly expanding and the scarcity of water resources is prominent in this region. In this study, Gravity Recovery and Climate Experiment (GRACE) and hydrological models were used to estimate the spatial-temporal changes of groundwater storage (GWS) and the driving factors of GWS variations were discussed in the 3H Plain. The results showed that GRACE-based GWS was depleted at a rate of -1.14 ± 0.89 cm/y in the 3H Plain during 2003 to 2015. The maximum negative anomaly occurred in spring due to agricultural irrigation activities. Spatially, the loss of GWS in the Haihe River Basin is more serious than that in the Huaihe River Basin, presenting a decreasing trend from south to north. Conversely, the blue water footprint (WFblue) of wheat exhibited an increasing trend from south to north. During the drought years of 2006, 2013, and 2014, more groundwater was extracted to offset the surface water shortage, leading to an accelerated decline in GWS. This study demonstrated that GWS depletion in the 3H Plain is well explained by reduced precipitation and groundwater abstraction due to anthropogenic irrigation activities.

3.
Bioorg Med Chem Lett ; 27(16): 3872-3877, 2017 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-28655423

RESUMO

Three novel structural series of 4″-O-(1-aralkyl-1,2,3-triazol-4-methyl-carbamoyl) azithromycin analogs were designed, synthesized and evaluated for their in vitro antibacterial activity. All the target compounds exhibited excellent activity against erythromycin-susceptible Streptococcus pyogenes, and significantly improved activity against three phenotypes of erythromycin-resistant Streptococcus pneumoniae compared with clarithromycin and azithromycin. Among the three series of azithromycin analogs, the novel series of 11,4″-disubstituted azithromycin analogs 9a-k exhibited the most effective and balanced activity against susceptible and resistant bacteria. Among them, compound 9j showed the most potent activity against Staphylococcus aureus ATCC25923 (0.008µg/mL) and Streptococcus pyogenes R2 (1µg/mL). Besides, all the 11,4″-disubstituted azithromycin analogs 9a-k except 9f shared the identical activity with the MIC value <0.002µg/mL against Streptococcus pyogenes S2. Furthermore, compounds 9g, 9h, 9j and 9k displayed significantly improved activity compared with the references against all the three phenotypes of resistant S. pneumoniae. Particularly, compound 9k was the most effective (0.06, 0.03 and 0.125µg/mL) against all the erythromycin-resistant S. pneumoniae expressing the erm gene, the mef gene and the erm and mef genes, exhibiting 2133, 133 and 2048-fold more potent activity than azithromycin, respectively.


Assuntos
Antibacterianos/farmacologia , Azitromicina/farmacologia , Escherichia coli/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Streptococcus pneumoniae/efeitos dos fármacos , Streptococcus pyogenes/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/química , Azitromicina/análogos & derivados , Azitromicina/síntese química , Azitromicina/química , Relação Dose-Resposta a Droga , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
4.
ChemMedChem ; 12(6): 420-425, 2017 03 17.
Artigo em Inglês | MEDLINE | ID: mdl-28195681

RESUMO

The treatment of the infections caused by Pseudomonas aeruginosa, an opportunistic Gram-negative bacterium, is very difficult. High intrinsic tolerance toward common antibiotics and the development of new resistant strains challenge us to find a new treatment as soon as possible. PqsD is an enzyme essential for the P. aeruginosa quorum-sensing apparatus, which catalyzes the final and key step in the biosynthesis of 4-hydroxy-2-heptylquinolone (HHQ), which is a signal molecule of the P. aeruginosa quorum-sensing system. In this review, following an outline on their structures, we present a brief introduction of the PqsD inhibitors including their mechanisms of action, inhibitory activity, and structure-activity relationships.


Assuntos
Anti-Infecciosos/química , Proteínas de Bactérias/antagonistas & inibidores , Percepção de Quorum/efeitos dos fármacos , Anti-Infecciosos/farmacologia , Proteínas de Bactérias/metabolismo , Benzoatos/química , Benzoatos/farmacologia , Ácidos Carboxílicos/química , Ácidos Carboxílicos/farmacologia , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/metabolismo , Quinolonas/química , Quinolonas/farmacologia , Relação Estrutura-Atividade
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