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1.
J Geophys Res Biogeosci ; 127(12): e2022JG007014, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37502709

RESUMO

Long-running eddy covariance flux towers provide insights into how the terrestrial carbon cycle operates over multiple timescales. Here, we evaluated variation in net ecosystem exchange (NEE) of carbon dioxide (CO2) across the Chequamegon Ecosystem-Atmosphere Study AmeriFlux core site cluster in the upper Great Lakes region of the USA from 1997 to 2020. The tower network included two mature hardwood forests with differing management regimes (US-WCr and US-Syv), two fen wetlands with varying levels of canopy sheltering and vegetation (US-Los and US-ALQ), and a very tall (400 m) landscape-level tower (US-PFa). Together, they provided over 70 site-years of observations. The 19-tower Chequamegon Heterogenous Ecosystem Energy-balance Study Enabled by a High-density Extensive Array of Detectors 2019 campaign centered around US-PFa provided additional information on the spatial variation of NEE. Decadal variability was present in all long-term sites, but cross-site coherence in interannual NEE in the earlier part of the record became weaker with time as non-climatic factors such as local disturbances likely dominated flux time series. Average decadal NEE at the tall tower transitioned from carbon source to sink to near neutral over 24 years. Respiration had a greater effect than photosynthesis on driving variations in NEE at all sites. Declining snowfall offset potential increases in assimilation from warmer springs, as less-insulated soils delayed start of spring green-up. Higher CO2 increased maximum net assimilation parameters but not total gross primary productivity. Stand-scale sites were larger net sinks than the landscape tower. Clustered, long-term carbon flux observations provide value for understanding the diverse links between carbon and climate and the challenges of upscaling these responses across space.

2.
Bioorg Med Chem ; 24(18): 4452-4463, 2016 09 15.
Artigo em Inglês | MEDLINE | ID: mdl-27480030

RESUMO

A facile and robust microwave-assisted solution phase parallel synthesis protocol was exercised for the development of a 38-member library of N,N'-disubstituted thiourea analogues (1-38) by using an identical set of conditions. The reaction time for synthesis of N,N'-disubstituted thiourea analogues was drastically reduced from a reported duration of 8-12h for conventional methods to only 1.5-2.0min. All the derivatives (1-38) were characterized by physico-analytical techniques such as elemental analysis in combination with FT-IR, (1)H, (13)C NMR and by single crystal XRD analysis have also been performed. These compounds were screened for their in vitro urease inhibition activities. Majority of compounds exhibited potent urease inhibition activities, however, the most significant activity was found for 16, with an IC50 value of 1.23±0.1µM. Furthermore, the synthesized compounds were screened for their cytotoxic potential against lungs cancer cell lines. Cell culture studies demonstrated significant toxicity of the compounds on the cell lines, and the levels of toxicity were altered in the presence of various side groups. The molecular docking studies of the most potent inhibitors were performed to identify the probable binding modes in the active site of the urease enzymes. These compounds have a great potential and significance for further investigations.


Assuntos
Clorobenzoatos/química , Micro-Ondas , Tioureia/análogos & derivados , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Linhagem Celular , Simulação por Computador , Cristalografia por Raios X , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Simulação de Acoplamento Molecular , Espectroscopia de Prótons por Ressonância Magnética , Espectroscopia de Infravermelho com Transformada de Fourier , Tioureia/farmacologia , Urease/antagonistas & inibidores , Urease/química
3.
Eur J Med Chem ; 70: 487-96, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24185379

RESUMO

An efficient and facile microwave-assisted solution phase parallel synthesis for a 26-member library of N,N'-disubstituted thiourea analogs were accomplished successfully. The reaction time for synthesis of analogs was drastically reduced from a reported 8-12 h to only 10 min. Compounds were more than 95% pure, as characterized by modern analytical techniques, i.e. (1)H &(13)C NMR and FT-IR. The solid phase structural analysis has also been performed by single crystal XRD analysis. Synthesized compounds were preliminary screened for their in vitro urease inhibition and antifungal activity. Most of the compounds were found to be potent inhibitors of urease. However, the most significant activity was found for 11 with IC50 of 1.67 µM. The docking scores correlate with the IC50 values of inhibitors.


Assuntos
Antifúngicos/farmacologia , Ácido Benzoico/química , Inibidores Enzimáticos/farmacologia , Micro-Ondas , Tioureia/farmacologia , Urease/metabolismo , Antifúngicos/síntese química , Antifúngicos/química , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Aspergillus/efeitos dos fármacos , Candida tropicalis/efeitos dos fármacos , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Testes de Sensibilidade Microbiana , Modelos Moleculares , Estrutura Molecular , Saccharomyces cerevisiae/efeitos dos fármacos , Soluções , Relação Estrutura-Atividade , Tioureia/análogos & derivados , Tioureia/síntese química
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