摘要：Based on the lead compound 1 reported in literature, a series of novel BACE1 inhibitors were designed and synthesized, among which compound 11 exhibited a 14-fold improvement in potency over the lead compound 1. This represents a good lead for the discovery of more promising BACE1 inhibitors for the potential treatment of AD.

摘要：By taking compound 1 as a lead, a series of 5-cyclopropyl substituted cyclic acylguanidine compounds were designed and synthesized as BACE1 inhibitors, compound 4d exhibited 84-fold improved inhibition efficiency than lead compound 1. The diphenyl fragment at the P3 position and the substituents at the second phenyl ring were essential for the compounds to achieve improved inhibition efficiency. This SAR studies provides new insights into the design and synthesis of more promising BACE1 inhibitors for the potential treatment of AD.

摘要：Based on the lead compounds 1 and 2, a series of novel BACE1 inhibitors were designed and synthesized,among which compound 9h exhibited a 60 fold improvement in potency over the lead compound 1. This represents a good lead for the discovery of more promising BACE1 inhibitors for the potential treatment of AD. The result also showed that the prop-2-yn-1-yloxy is a suitable fragment for modification of cyclic acylguanidine BACE1 inhibitors.

摘要：随着电动汽车、光伏发电等越来越多的新型电网交互型设备接入楼宇,以往的楼宇变电站难以处理复杂的能量流动,导致能量传递效率降低、接口复杂化和电能质量变差的现象。为此,提出一种无线电能路由器与电能质量控制方法。首先,为设计高效的能量流动控制方法,提出无线电能路由器构成的等效模型;其次,为了在所有负载、电能质量情况中保持高效的能量流动,对不同负载、电能质量情况进行分类并给出相应的控制参考量;随后,基于所有分类的控制参考量,设计对不同负载、电能质量情况下的功率控制方法;最后,为验证所提结构和控制方法的可行性,设计相对应情况的仿真案例。所提无线电能路由器可以为楼宇提供一种统一接入电网交互型设备的解决方案,具有重要的工程意义。

摘要：目的 :设计一种新型动物口腔诊疗支架,并将其应用于犬牙髓再生实验。方法 :该装置包括上支撑架、口腔限位架和下支撑架3个部分,并依上至下相连接。上、下支撑架高度和宽度为可调节式,且支撑架可旋转,末端为弧形结构。口腔限位架左右两侧为套筒结构,连接套筒结构的上限位杆与下支撑架中的下限位杆为可伸缩式。结果:该口腔诊疗支架能使实验动物稳定维持长时间的张口状态,并可根据不同种类动物的颌面部结构进行三维调整,方便医护人员对动物进行喉部检查、口腔检查、口腔护理及牙科治疗(如根管治疗、牙体充填)和其他医护行为。结论:该口腔诊疗支架设计合理、结构简单、便于携带,方便拆卸与组装,易于消毒与灭菌,且成本低廉,可以起到保护软组织、开放手术视野、隔离唾液污染的作用,值得在临床动物实验以及动物诊所推广使用。

摘要：《愤怒的葡萄》是美国 2 0世纪 3 0年代大萧条时期的一部史诗性的作品。这部作品不仅在题材上具有独特性 ,而且在艺术结构方面也匠心独运 ,它改变了以前单一的平面结构 ,采用了叙事章与插入章相结合的手法。本文试图探讨的是插入章在作品中的作用及表达方式。

摘要：以白千层树皮为原料,探究了超级电容器电极用树皮活性炭(bark activated carbon,BAC)的制备工艺。通过正交试验设计,确定了最佳制备条件:KOH活化,炭化温度600℃,活化温度700℃,炭碱质量比1∶4。所制备的BAC展现出较好的电化学性能。在0.2 A/g电流密度下,其比容量达284 F/g,4 000次恒流充放电后的库伦效率为103%。活化后,试样的比表面积由142.35 m^(2)/g增至2 052.29 m^(2)/g,石墨化程度提高,电阻降低,导电性增加,电化学性能增强。本研究拓宽了白千层树皮的应用领域,为其废弃物的回收再利用提供了新路径。

摘要：It is well-known that global warming due to anthropogenic atmospheric greenhouse effects advanced the start of the vegetation growing season （SOS） across the globe during the 20th century. Projections of further changes in the SOS for the 21st century under certain emissions scenarios （Representative Concentration Pathways, RCPs） are useful for improving understanding of the consequences of global warming. In this study, we first evaluate a linear relationship between the SOS （defined using the normalized difference vegetation index） and the April temperature for most land areas of the Northern Hemisphere for 1982-2008. Based on this relationship and the ensemble projection of April temperature under RCPs from the latest state-of-the-art global coupled climate models, we show the possible changes in the SOS for most of the land areas of the Northern Hemisphere during the 21st century. By around 2040-59, the SOS will have advanced by -4.7 days under RCP2.6, -8.4 days under RCP4.5, and -10.1 days under RCPS.5, relative to 1985-2004. By 2080-99, it will have advanced by -4.3 days under RCP2.6, -11.3 days under RCP4.5, and -21.6 days under RCP8.5. The geographic pattern of SOS advance is considerably dependent on that of the temperature sensitivity of the SOS. The larger the temperature sensitivity, the larger the date-shift-rate of the SOS.

摘要：主泵惯量设计应考虑主泵本身和回路特性的综合影响。本文建立了基于四象限特性的主泵惰转数值计算模型,评估主泵本身和回路特性对主泵惰转的影响。结果表明,转动惯量、摩擦损失等主泵因素,沿程阻力、局部阻力等回路因素均影响主泵惰转流量特性,但惰转转速下降主要与主泵本身因素相关,与回路因素关系不大。采用初始动能比ε表征主泵惯性和回路流体惯性的综合影响,流量下降相对转速下降的滞后程度与ε线性相关。对于ε较大的回路,应充分考虑惰转流量的滞后影响,避免主泵转动惯量设计采用过大的裕量,造成机组效率下降和设计难度提高。

摘要：Projections of potential submerged area due to sea level rise are helpful for improving understanding of the influence of ongoing global warming on coastal areas. The Ensemble Empirical Mode Decomposition method is used to adaptively decompose the sea level time series in order to extract the secular trend component. Then the linear relationship between the global mean sea level （GMSL） change and the Zhujiang （Pearl） River Delta （PRD） sea level change is calculated： an increase of 1.0 m in the GMSL corresponds to a 1.3 m （uncertainty interval from 1.25 to 1.46 m） increase in the PRD. Based on this relationship and the GMSL rise projected by the Coupled Model Intercomparison Project Phase 5 under three greenhouse gas emission scenarios （representative concentration pathways, or RCPs, from low to high emission scenarios RCP2.6, RCP4.5, and RCP8.5）, the PRD sea level is calculated and projected for the period 2006-2100. By around the year 2050, the PRD sea level will rise 0.29 （0.21 to 0.40） m under RCP2.6, 0.31 （0.22 to 0.42） m under RCP4.5, and 0.34 （0.25 to 0.46） m under RCP8.5, respectively. By 2100, it will rise 0.59 （0.36 to 0.88） m, 0.71 （0.47 to 1.02） m, and 1.0 （0.68 to 1.41） m, respectively. In addition, considering the extreme value of relative sea level due to land subsidence （i.e., 0.20 m） and that obtained from intermonthly variability （i.e., 0.33 m）, the PRD sea level will rise 1.94 m by the year 2100 under the RCP8.5 scenario with the upper uncertainty level （i.e., 1.41 m）. Accordingly, the potential submerged area is 8.57x103 km2 for the PRD, about 1.3 times its present area.