A series of novel human enterovirus 71 inhibitors, N-benzyl-N-phenylthiophene-2-carboxamide analogues, were synthesized and their antiviral activities were evaluated in vitro. Most derivatives of this structure agains...
详细信息
A series of novel human enterovirus 71 inhibitors, N-benzyl-N-phenylthiophene-2-carboxamide analogues, were synthesized and their antiviral activities were evaluated in vitro. Most derivatives of this structure against EV71 had a low micromolar range in the RD (rhabdomyosarcoma) cell lines. The most potent compound 5a, N-(4-bromobenzyl)-N-(4-fluorophenyl) thiophene-2-carboxamide, showed low micromolar activity against EV71 (EC50 = 1.42 mu M) compared to the reference anti-EV71 drug enviroxime (EC50 = 0.15 mu M). Preliminary SAR studies revealed that the thiophene-2-carboxamide core is crucial for maintaining antiviral activity, and N-substituent phenyl groups largely influenced the anti-EV71 efficacy of this new class of potent antiviral agents.
Fresh water for human daily life is an important resource of the world, which could be as precious as oil in many cases. The increased needs for fresh water are becoming a major challenge to the quality of our life. R...
详细信息
Fresh water for human daily life is an important resource of the world, which could be as precious as oil in many cases. The increased needs for fresh water are becoming a major challenge to the quality of our life. Recently much attention has been paid to the seawater desalination with low energy cost. Here we report a seawater desalination (SD) and electrolysis (SE) system on the basis of the newly invented triboelectric nanogenerator (TENG). The TENG consists of radial arrays of micro-sized sectors on the contact surfaces and exhibits a high output current of 3.3 mA. 0.5 M salt solution was desalinated to form drinking water in 16 h and the desalination rate reached 98.3%. Subsequently, a totally self-powered SD and SE system driven by the kinetic energy of flowing water was presented. Using the power generated by flowing water at a rate of 40 L min(-1), the desalination rate reaches 8.2% in 3 h. Furthermore, the byproduct of concentrated salty water was split at a hydrogen production rate of 2.6 x 10(-5) mL s(-1). Our study demonstrates an innovative and unique approach toward a total self-powered SD and SE system. This is an important step toward self-powered environmental electrochemistry. (C) 2015 Published by Elsevier Ltd.
In this work, we report the synthesis of dye-loaded and folic acid (FA)-conjugated organically modified silica (ORMOSIL) nanoparticles as targeted optical nanoprobes for in vitro and in vivo imaging. The dye-loaded OR...
详细信息
In this work, we report the synthesis of dye-loaded and folic acid (FA)-conjugated organically modified silica (ORMOSIL) nanoparticles as targeted optical nanoprobes for in vitro and in vivo imaging. The dye-loaded ORMOSIL (ORMD) nanoparticles are synthesized by a facile aqueous phase (oil-in-water microemulsion) approach and they have an average size of 30 nm. We observed that the functionalization of FA onto the particle surface led to a strong cellular uptake of FA-conjugated ORMD nanoparticles for pancreatic cancer Miapaca-2 cells and hepatoma SMMC7721 cells with FA receptor overexpression. Such a trend is not observed for 293T cells and breast cancer MCF7 cells as these cells possess low-expression of the FA receptor. The in vivo imaging studies demonstrate that FA-ORMD nanoparticles are preferentially accumulated in tumor sites. Histological studies reveal that no-ill effects are observed in the major organs of treated mice when compared to the untreated ones. Because of the facile synthesis process, high specificity for tumor targeting and low toxicity of FA-ORMD nanoparticles, significant potential for early-cancer detection application is expected.
A series of methyl ursolate 3-O-beta-chacotrioside analogs have been designed, synthesized and evaluated as H5N1 entry inhibitors based on a small molecule inhibitor saponin 3 previously discovered by us. Detailed str...
详细信息
A series of methyl ursolate 3-O-beta-chacotrioside analogs have been designed, synthesized and evaluated as H5N1 entry inhibitors based on a small molecule inhibitor saponin 3 previously discovered by us. Detailed structure-activity relationships (SARs) studies on the aglycone of compound 3 indicated that both the type of pentacyclic triterpene and the subtle modification of ursolic acid as an aglycon had key influences on the antiviral activity. These results suggested that either the introduction of a disubstituted amide structure at the 17-COOH of ursolic acid or alteration of the C-3 configuration of ursolic acid from 3 beta-to 3 alpha-forms was helpful to significantly improve the selective index while keeping their antiviral activities. (C) 2015 Elsevier Masson SAS. All rights reserved.
暂无评论