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A series of novel naphthalimide aminothiazoles were developed for the first time and evaluated for their antimicrobial activity. Some prepared compounds possessed good inhibitory activity against the tested bacteria and fungi. Noticeably, the piperazine derivative displayed superior antibacterial activity against MRSA and with MIC values of 4 and 8 μg/mL, respectively, to reference drugs. The most active compound showed low toxicity against mammalian cells with no obvious triggering of the development of bacterial resistance, and it also possessed rapid bactericidal efficacy and efficient membrane permeability. Preliminarily investigations revealed that compound could not only bind with gyrase-DNA complex through hydrogen bonds but could effectively intercalate into MRSA DNA to form -DNA supramolecular complex, which might be responsible for the powerful bioactivity. Further transportation behavior evaluation indicated that molecule could be effectively stored and carried by human serum albumin, and the hydrophobic interactions and hydrogen bonds played important roles in the binding process.

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Temporal trends of total liver cancer have been well reported in China, especially the trends caused by hepatitis B (HBV); however, the trends of liver cancer attributable to specific etiologies have rarely been reported in China. Thus, this study aims to describe the temporal trends in the incidence, mortality and DALYs of total and etiology-specific liver cancer in China from 1990 to 2019. We extracted the incidence, mortality and disability-adjusted life years (DALYs) of total and etiology-specific liver cancer in China from 1990 to 2019 from global disease burden (GBD) 2019. We plotted the trends in the age-standardized rates for incidence, mortality, and DALYs using locally weighted regression (LOESS)-smoothed data from 1990 to 2019. The age-standardized rate for the incidence of liver cancer was analyzed with an age-period-cohort method. The age-standardized rates for incidence, death, and DALYs decreased by −58.8%, −63.8%, and −65.6%, respectively, between 1990 and 2019. The age-standardized rates of incidence, mortality, and DALYs of total liver cancer showed similar temporal patterns, presenting an overall decline, with the average annual percentage change (AAPC) ranging from −3.3% to −3.8%. People in the period before 2007 had a higher risk, and people after 2007 had a lower risk. The cohort risk ratios (RRs) showed decreasing patterns, with the most rapid decline observed in the 1910 to 1960 cohorts. Our study generally revealed favorable decreasing trends for total and etiology-specific liver cancer in China from 1990 to 2019. Despite the overall decline in liver cancer due to heavy alcohol use and obesity from 1990 to 2019, there have been apparent upward trends since 2006. Planned population-wide interventions targeting heavy alcohol use and obesity may mitigate the increasing trends in liver cancer attributable to alcohol use and NASH.

Lightning shielding failure accounts for the most proportion of the lightning accident for transmission systems above 500 kV. The leader propagation model (LPM) was found to be effective to the analysis of lightning shielding failure of high voltage transmission lines, especially for the ultra-high voltage (UHV) transmission systems. However, it was generally inefficient to calculate the shielding failure rate by LPM since the progress of lightning development must be simulated repeatedly which is time consuming and no adaptive implementation of LPM has been reported. In this paper, adaptive strategies to accelerate the computation of shielding failure analysis by LPM were proposed, which include the adaptive time step control according to the electric field at the conductor surface, non-uniform lightning current sampling based on the lightning current amplitude probability distribution, and adaptive lightning location sampling based on recursive adaptive Simpson's method. The analysis results was validated by the field data of the UHV transmission line in Japan, and the efficiency of the adaptive strategies was shown by the shielding failure analysis of a typical 500kV AC transmission line.Index Terms-Adaptive strategy, leader propagation model, lightning shielding failure, lightning protection, transmission line.

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