Discovery of N-arylsulfonyl-3-acylindole benzoyl hydrazone derivatives as anti-HIV-1 agents

The discovery and development of novel inhibitors with activity against variants of human immunodeficiency virus type 1 (HIV-1) is pivotal for overcoming treatment failure. As our ongoing work on research of anti-HIV-1 inhibitors, 32 N-arylsulfonyl-3-acylindole benzoyl hydrazone derivatives were prepared by introduction of the hydrazone fragments on the N-arylsulfonyl-3-acylindolyl skeleton and preliminarily screened in vitro as HIV-1 inhibitors for the first time. Among of all the reported analogues, eight compounds exhibited significant anti-HIV-1 activity, especially N-(3-nitro)phenylsulfonyl-3- acetylindole benzoyl hydrazone (18) and N-(3-nitro)phenylsulfonyl-3-acetyl-6-methylindole benzoyl hydrazone (23) displayed the most potent anti-HIV-1 activity with EC50 values of 0.26 and 0.31 μg/mL, and TI values of >769.23 and >645.16, respectively. It is noteworthy that introduction of R3 as the methyl group and R2 as the hydrogen group could result in more potent compounds. This suggested that introduction of R3 as the methyl group could be taken into account for further preparation of these kinds of compounds as anti-HIV-1 agents

Optimizing the Coverage via the UAVs With Lower Costs for Information-Centric Internet of Things

The recent developments in the areas of the Internet of Things (IoTs) have provided a rapid growth in the epoch of the novel information-centric collections (IC-IoTs). In the IC-IoTs, expanding the ranges of information collections and reducing the costs are important issues for the information required platform. In the previous scenarios, the information is collected in a random manner, which leads to lower coverages and higher costs. Thus, a "optimizing the coverage via the unmanned aerial vehicles (UAVs) with lower costs for information-centric Internet of Things" (OCLC-IoTs) approach is established, which targets to improve the coverage ratio and to reduce the costs of the information-required platform via the cooperation of the information collectors and the UAVs. First, to improve the coverage ratio, an intensive strategy is proposed to inspire the information collectors to bid for the tasks published by the platform and an improved rolling horizon strategy (IRHS) strategy is designed to plan the flying routes of the UAVs to reach more coverage ranges. Then, to reduce the costs factor, the IRHS strategy is designed to shorten the flying routes of the UAVs under the prerequisite of guaranteeing coverage ratio to achieve fewers costs. Finally, a comprehensive theoretical analysis and experiments are provided, which indicates the advancements of the OCLC-IoTs scheme. Compared with the previous studies, the OCLC-IoTs scheme can improve the coverage ratio of information by 21.42% approximately and can reduce the cost ratio by 13.335% to 34.32%

KIN10 promotes stomatal development through stabilization of the SPEECHLESS transcription factor

Stomata are epidermal structures that modulate gas exchanges between plants and the atmosphere. The formation of stomata is regulated by multiple developmental and environmental signals, but how these signals are coordinated to control this process remains unclear. Here, we showed that the conserved energy sensor kinase SnRK1 promotes stomatal development under short-day photoperiod or in liquid culture conditions. Mutation of KIN10, the catalytic α-subunit of SnRK1, results in the decreased stomatal index; while overexpression of KIN10 significantly induces stomatal development. KIN10 displays the cell-type-specific subcellular location pattern. The nuclear-localized KIN10 proteins are highly enriched in the stomatal lineage cells to phosphorylate and stabilize SPEECHLESS, a master regulator of stomatal formation, thereby promoting stomatal development. Our work identifies a module links connecting the energy signaling and stomatal development and reveals that multiple regulatory mechanisms are in place for SnRK1 to modulate stomatal development in response to changing environments

Effect of Pnictogen Height on Spin Waves in Iron Pnictides

We use inelastic neutron scattering to study spin waves in the antiferromagnetic ordered phase of iron pnictide NaFeAs throughout the Brillouin zone. Comparing with the well-studied AFe2As2 (A=Ca, Sr, Ba) family, spin waves in NaFeAs have considerably lower zone boundary energies and more isotropic effective in-plane magnetic exchange couplings. These results are consistent with calculations from a combined density functional theory and dynamical mean field theory and provide strong evidence that pnictogen height controls the strength of electron-electron correlations and consequently the effective bandwidth of magnetic excitations

Dynamic placement of the linker histone H1 associated with nucleosome arrangement and gene transcription in early Drosophila embryonic development

The linker histone H1 is critical to maintenance of higher-order chromatin structures and to gene expression regulation. However, H1 dynamics and its functions in embryonic development remain unresolved. Here, we profiled gene expression, nucleosome positions, and H1 locations in early Drosophila embryos. The results show that H1 binding is positively correlated with the stability of beads-on-a-string nucleosome organization likely through stabilizing nucleosome positioning and maintaining nucleosome spacing. Strikingly, nucleosomes with H1 placement deviating to the left or the right relative to the dyad shift to the left or the right, respectively, during early Drosophila embryonic development. H1 occupancy on genic nucleosomes is inversely correlated with nucleosome distance to the transcription start sites. This inverse correlation reduces as gene transcription levels decrease. Additionally, H1 occupancy is lower at the 5\u27 border of genic nucleosomes than that at the 3\u27 border. This asymmetrical pattern of H1 occupancy on genic nucleosomes diminishes as gene transcription levels decrease. These findings shed new lights into how H1 placement dynamics correlates with nucleosome positioning and gene transcription during early Drosophila embryonic development

No Consistent Simulated Trends in the Atlantic Meridional Overturning Circulation for the Past 6,000 Years

The Atlantic Meridional Overturning Circulation (AMOC) is a key feature of the North Atlantic with global ocean impacts. The AMOC's response to past changes in forcings during the Holocene provides important context for the coming centuries. Here, we investigate AMOC trends using an emerging set of transient simulations using multiple global climate models for the past 6,000 years. Although some models show changes, no consistent trend in overall AMOC strength during the mid-to-late Holocene emerges from the ensemble. We interpret this result to suggest no overall change in AMOC, which fits with our assessment of available proxy reconstructions. The decadal variability of the AMOC does not change in ensemble during the mid- and late-Holocene. There are interesting AMOC changes seen in the early Holocene, but their nature depends a lot on which inputs are used to drive the experiment