随着智能电网建设和数字化转型的推进,变电站出现了以机器人巡检、移动作业、物联网数据采集为代表的新型业务,这些业务总体呈现出大带宽、高移动、大连接特点,变电站亟需建设覆盖全站的无线网络,为变电站无线高清视频监控、巡检机器人...随着智能电网建设和数字化转型的推进,变电站出现了以机器人巡检、移动作业、物联网数据采集为代表的新型业务,这些业务总体呈现出大带宽、高移动、大连接特点,变电站亟需建设覆盖全站的无线网络,为变电站无线高清视频监控、巡检机器人、移动办公和作业、远程调度、应急通信等以及其它智能化监测监控系统应用提供终端部分的无线接入通道,解决高带宽业务的安全可靠接入和各类智能感知业务最后一公里通信需求。WAPI(WLAN Authentication and Privacy Infrastructure)技术具有组网灵活、网络扩展性好、融合性好、兼容性高、通信速率高以及与互联网对接方便等优点,更重要的是其安全性高,可实现变电站建设无线WAPI局域网便能满足各类智能化监测监控系统对无线接入的需求。展开更多
Based on the strategies of receptor structure-guided neonicotinoid design, a series of novel cis-nitenpyram analogues bearing diglycine esters were designed and synthesized. Preliminary bioassays indicated that the in...Based on the strategies of receptor structure-guided neonicotinoid design, a series of novel cis-nitenpyram analogues bearing diglycine esters were designed and synthesized. Preliminary bioassays indicated that the insecticidal spectra of the target compounds were expanded compared with our previous work, while all the target compounds presented excellent insecticidal activities against Nilaparvata lugens and Aphis medicagini at 100 mg/L. Among these analogues, 6b showed 100% mortality against Nilaparvata lugens (LC 50 = 0.163 mg/L) and 90% against Aphis medicagini at 4 mg/L. SARs suggested that the insecticidal potency of our designed cis-nitenpyram analogues was dual-controlled by the size and species of the ester groups. The molecular docking simulations revealed that the structural uniqueness of these analogues may lead to a unique molecular recognition and binding mode compared with the previously designed compounds. Introduction of the peptide bond gave rise to more significant hydrogen bonds between the nitenpyram analogues bonding with the amino acid residues of insect nAChRs. The docking results explained the SARs observed in vitro, and shed light on the novel insecticidal mechanism of these cis-nitenpyram analogues.展开更多
To make further studies on the difference of cis-nitenpyram analogues, a series of cis-nitenpyram com- pounds containing a flexible amido segment anchored on tetrahydropyrimidine ring was designed and synthesized. Pre...To make further studies on the difference of cis-nitenpyram analogues, a series of cis-nitenpyram com- pounds containing a flexible amido segment anchored on tetrahydropyrimidine ring was designed and synthesized. Preliminary bioassays indicate that all the analogues exhibit a mortality of 100% at 100 rag/L, and the analogue 4d shows the best activity against Nilaparvata lugens and Myzus persicae, with a mortality of 100% at 4 mg/L （LCs0=0.172 rag/L）. The structure activity relationship studies show that insecticidal activities of the analogues are affected by the kinds and size of substituent R. In addition, the molecular docking simulations reveal that compouds 4 with a flexible amido segment on tetrahydropyrimidine ring show their different binding affinities for the nicotinic acetyleholine receptor（nAChR） of insect and compoud 4d shows stronger hydrogen-bonding with nAChR, which may provide the structure-activity relationship observed in vitro.展开更多
A series of novel 2H-pyrazolo[4,3-c]hexahydropyridine derivatives （II） have been designed and synthesized. The target com- pounds have been identified by elemental analysis and spectral （1H NMR, IR, and MS） data a...A series of novel 2H-pyrazolo[4,3-c]hexahydropyridine derivatives （II） have been designed and synthesized. The target com- pounds have been identified by elemental analysis and spectral （1H NMR, IR, and MS） data and the absolute configuration of compound （IIl） was confirmed by single crystal X-ray diffraction. The cytotoxicity of the target compounds have been evalu- ated in vitro against two human breast cancer cell lines MCF-7 and MDA-MB-231 by MTT assay. Most compounds exhibited good inhibition, and compounds II21 （IC50 = 4.7 μM for MCF-7 and IC50 = 9.3 μM for MDA-MB-231）, 1133 （IC50 = 2.4 μM for MCF-7 and IC50 = 4.2 gM for MDA-MB-231） and 114o （IC50 = 3.3 μM for MCF-7 and IC5o =8.6 μM for MDA-MB-231） dis- played better inhibitory activity than 5-fluorouracil （IC50 = 4.8 μM for MCF-7 and IC50 = 9.6 I, tM for MDA-MB-231, respec- tively）. Flow cytometric analysis and DNA fragmentation suggest that II33 is cytotoxic and able to induce the apoptosis of MCF-7 cells. The fluorescence properties of compounds IIl, II6, II11,II16, II23, Il2s, and II3s were also studied and compound Ilzs afforded the highest photoluminescence quantum yield （38%）.展开更多
文摘随着智能电网建设和数字化转型的推进,变电站出现了以机器人巡检、移动作业、物联网数据采集为代表的新型业务,这些业务总体呈现出大带宽、高移动、大连接特点,变电站亟需建设覆盖全站的无线网络,为变电站无线高清视频监控、巡检机器人、移动办公和作业、远程调度、应急通信等以及其它智能化监测监控系统应用提供终端部分的无线接入通道,解决高带宽业务的安全可靠接入和各类智能感知业务最后一公里通信需求。WAPI(WLAN Authentication and Privacy Infrastructure)技术具有组网灵活、网络扩展性好、融合性好、兼容性高、通信速率高以及与互联网对接方便等优点,更重要的是其安全性高,可实现变电站建设无线WAPI局域网便能满足各类智能化监测监控系统对无线接入的需求。
基金supported by the National Natural Science Foundation of China (21042010, 21102092 and 30870560)the Key Scientific "Twelfth Five-Year" National Technology Support Program (2011BAE06B01-17)+3 种基金the Key Project of Science and Technology Commission of Shanghai (105405503400)the Innovation Project of Shanghai Education Commission (12YZ078)the Leading Academic Discipline Project of Shanghai Normal University (DZL808)Shanghai Key Laboratory of Rare Earth Functional Materials, Shanghai Normal University (07dz22303)
文摘Based on the strategies of receptor structure-guided neonicotinoid design, a series of novel cis-nitenpyram analogues bearing diglycine esters were designed and synthesized. Preliminary bioassays indicated that the insecticidal spectra of the target compounds were expanded compared with our previous work, while all the target compounds presented excellent insecticidal activities against Nilaparvata lugens and Aphis medicagini at 100 mg/L. Among these analogues, 6b showed 100% mortality against Nilaparvata lugens (LC 50 = 0.163 mg/L) and 90% against Aphis medicagini at 4 mg/L. SARs suggested that the insecticidal potency of our designed cis-nitenpyram analogues was dual-controlled by the size and species of the ester groups. The molecular docking simulations revealed that the structural uniqueness of these analogues may lead to a unique molecular recognition and binding mode compared with the previously designed compounds. Introduction of the peptide bond gave rise to more significant hydrogen bonds between the nitenpyram analogues bonding with the amino acid residues of insect nAChRs. The docking results explained the SARs observed in vitro, and shed light on the novel insecticidal mechanism of these cis-nitenpyram analogues.
文摘To make further studies on the difference of cis-nitenpyram analogues, a series of cis-nitenpyram com- pounds containing a flexible amido segment anchored on tetrahydropyrimidine ring was designed and synthesized. Preliminary bioassays indicate that all the analogues exhibit a mortality of 100% at 100 rag/L, and the analogue 4d shows the best activity against Nilaparvata lugens and Myzus persicae, with a mortality of 100% at 4 mg/L （LCs0=0.172 rag/L）. The structure activity relationship studies show that insecticidal activities of the analogues are affected by the kinds and size of substituent R. In addition, the molecular docking simulations reveal that compouds 4 with a flexible amido segment on tetrahydropyrimidine ring show their different binding affinities for the nicotinic acetyleholine receptor（nAChR） of insect and compoud 4d shows stronger hydrogen-bonding with nAChR, which may provide the structure-activity relationship observed in vitro.
基金supported by Zooblast-molecular Biology Laboratory of Shanghai Normal Universitysupported by the National Natural Science Foundation of China (21042010, 21102092 and30870560)+4 种基金the Key Scientific "Twelfth Five-Year" National Technology Support Program (2011BAE06B01-17)the Innovation Project of Shanghai Education Commission (12YZ078)the Key Project of the Science and Technology Commission of Shanghai 105405503400)the Leading Academic Discipline Project of Shanghai Normal University (DZL808)Shanghai Key Laboratory of Rare Earth Functional Materials, Shanghai Normal University (07dz22303)
文摘A series of novel 2H-pyrazolo[4,3-c]hexahydropyridine derivatives （II） have been designed and synthesized. The target com- pounds have been identified by elemental analysis and spectral （1H NMR, IR, and MS） data and the absolute configuration of compound （IIl） was confirmed by single crystal X-ray diffraction. The cytotoxicity of the target compounds have been evalu- ated in vitro against two human breast cancer cell lines MCF-7 and MDA-MB-231 by MTT assay. Most compounds exhibited good inhibition, and compounds II21 （IC50 = 4.7 μM for MCF-7 and IC50 = 9.3 μM for MDA-MB-231）, 1133 （IC50 = 2.4 μM for MCF-7 and IC50 = 4.2 gM for MDA-MB-231） and 114o （IC50 = 3.3 μM for MCF-7 and IC5o =8.6 μM for MDA-MB-231） dis- played better inhibitory activity than 5-fluorouracil （IC50 = 4.8 μM for MCF-7 and IC50 = 9.6 I, tM for MDA-MB-231, respec- tively）. Flow cytometric analysis and DNA fragmentation suggest that II33 is cytotoxic and able to induce the apoptosis of MCF-7 cells. The fluorescence properties of compounds IIl, II6, II11,II16, II23, Il2s, and II3s were also studied and compound Ilzs afforded the highest photoluminescence quantum yield （38%）.
