RESUMO
A new series of simplified azasordarin analogs was synthesized using as key steps a Diels-Alder reaction to generate a highly substituted bicyclo[2.2.1]heptane core, followed by a subsequent nitrile alkylation. Several additional strategies were investigated for the generation of the key tertiary nitrile or aldehyde thought to be required for inhibition at the fungal protein eukaryotic elongation factor 2. This new series also features a morpholino glycone previously reported in semisynthetic sordarin derivatives with broad spectrum antifungal activity. Despite a lack of activity against Candida albicans for these early de novo analogs, the synthetic route reported here permits more comprehensive modifications of the bicyclic core and structure-activity relationship studies that were not heretofore possible.
Assuntos
Antifúngicos/síntese química , Antifúngicos/farmacologia , Indenos/síntese química , Indenos/farmacologia , Alcenos/química , Antifúngicos/química , Antifúngicos/metabolismo , Técnicas de Química Sintética , Fator de Iniciação 2 em Eucariotos/química , Fator de Iniciação 2 em Eucariotos/metabolismo , Indenos/química , Indenos/metabolismo , Simulação de Acoplamento Molecular , Nitrilas/química , Conformação ProteicaRESUMO
The study analyzes the survey data on the surface sediments in 355 stations in Xiamen Sea area during 2004-2006, 2007-2009, 2010-2013, and 2014-2016. The result finds that contents of TOC, sulfide, and oils in the surface sediments were generally low but showed significant spatial differences (p < 0.05) in most cases, with TOC in the West Sea area (WS) staying significantly higher than other sea areas. Xiamen Sea area suffered universal heavy metal pollution mainly from Cu and Zn for years in the WS, the Jiulong River Estuary (JE), and the East Sea area (ES), and the heavy metal pollution index (HPI) exhibited significant spatial differences across the four periods (p < 0.05). With the source of heavy metals in the WS being mainly related to human activities, Cu and Zn were related to the development of port shipping and Pb to aquaculture. The heavy metal pollution in JE was mainly related to the input of rivers emptying into the sea. The high Cu content in the ES was related to the direct discharge of massive domestic sewage into the sea at the time. From 2004 to 2016, the potential ecological risks of heavy metals in Xiamen Sea area stayed low.
Assuntos
Metais Pesados , Poluentes Químicos da Água , China , Monitoramento Ambiental , Sedimentos Geológicos , Humanos , Chumbo , Metais Pesados/análise , Óleos , Medição de Risco , Rios , Esgotos , Sulfetos , Poluentes Químicos da Água/análiseRESUMO
The types and intensity of anthropogenic pressure in the same sea area may differ spatially and may change as time passes, but response of benthic biotic indices to different pressure is different, which makes it unreasonable to use the same benthic biotic indices in a large sea area. We provided a new way of thinking as to selecting benthic biotic indices according to pressure type. The study took six bays under eutrophication and sediment heavy metal pollution to different levels in Fujian coastal water, East China sea, as examples, analysed the response of five benthic biotic indices, namely AZTI marine biotic index (AMBI), multivariate AMBI (M-AMBI), Shannon-Wiener diversity index (H'), benthic opportunistic polychaetes amphipods (BOPA) and benthic polychaetes amphipods (BPA), to eutrophication factors and sediment heavy metal pollution factors firstly. The result indicated that AMBI well responded to dissolved inorganic nitrogen (DIN) and dissolved inorganic phosphorus (DIP); M-AMBI responded soundly in the range of DIN >0.131 mg L-1 and DIP >0.022 mg L-1 and responded universally to heavy metals; H' responded to only Hg and Cd; BOPA has response to eutrophication condition of DIN >0.242 mg L-1; BPA had response to DIN, Cu and As. Then, suitable indices were selected based on the four pressure scenarios in the study area. AMBI was selected in no pressure scenario; M-AMBI was chosen under only eutrophication pressure and under dual pressure; H' was preferred in only heavy metal pressure scenario (mainly Hg pollution). At last, the density plot of the distribution of the selected indices in the evaluation grades under different pressure scenarios proved the proposal of selecting benthic biotic indices according to pressure types feasible. This study can offer some new insights into rapidly choosing indices to evaluate the coastal benthic ecological quality status.
Assuntos
Anfípodes , Mercúrio , Animais , Cádmio , China , Ecossistema , Monitoramento Ambiental , Eutrofização , Invertebrados , Nitrogênio , Fósforo , ÁguaRESUMO
A concise and stereoselective synthesis of the trioxadispiroketal motif that embodies the DEF-ring of the marine macrolide (+)-spirastrellolide A is described. The synthetic approach features a sequence of cyclic acetal tethered ring-closing metathesis and Suárez oxidative cyclization, thereby constituting a viable strategy for constructing the Northern Half.