摘要：In order to find novel antifungal agents with good activity and aqueous solubility, a series of SYN-2869 analogues containing a pyridine ring were synthesized and evaluated for their in vitro antifungal activity and water solubility. The results indicated that some compounds showed potent activity against six pathogenic fungi. In particular, the analogue 17a having an isobutyl substitution on the triazolone exhibited significant broad spectrum antifungal activity. In addition, the water solubility of compound l？a was sufficiently improved over SYN-2869.

摘要：A series of novel triazole derivatives containing y-lactam were designed and synthesized, and their structures were confirmed by IH NMR, 13C NMR and HRMS, The in vitro antifungal activities of the target compounds were evaluated, The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2A and CYP51 was investigated.

摘要：Based on the active site of Candida albicans lanosterol 14α-demethylase (CACYP51), novel triazole compounds structurally different from the current triazole drugs were designed and synthesized. In vitro antifungal activities showed that compounds 10, 11, 16 and 20 exhibited strong activities. In addition, compounds 10, 11 and 16 also displayed certain activities against fluconazole-resistant fungi.

摘要：Based on the active site of Aspergillus fumigatus lanosterol 14α-demethylase （AF-CYP51）, novel triazole compounds were designed. Their chemical synthesis and the antifungal activities were reported. The results showed that all the target compounds exhibited excellent activities with broad spectrum; in which compounds 4, 12 and 15 showed comparable activities against A. fumigatus to the control drug itraconazole.

摘要：Energetic particle radiation diagnoses mainly detect the particles(such as neutrons,gamma rays,hard X-rays,and escaping electrons)that are radiated in the discharge process of the experimental advanced superconducting tokamak device to characterize the operating state of the plasma in real *** upgrading of these diagnoses requires new instruments based on national(here,“national”means developed and produced by a Chinese company)core chips and open-source software with advanced digitization,a high sampling rate,and a high time *** new spectroscopy system designed in this study adopts the national field-programmable gate array(FPGA)and an analog-to-digital converter as the core chip,and it is developed using Qt on *** communication between the FPGA and embedded controller occurs via a high-speed peripheral component interconnect eXtension for instrument express protocol with a direct memory access *** this basis,the time resolution of the system is improved from 2 to 1 ms,the maximum channel address is increased to 4096,and the sampling rate is increased from 10 to 80 *** experiments of the spectroscopy system with 152Eu and 137Cs sources demonstrate that the best energy resolution is 0.27%and the measurement error is less than±0.5 keV.

摘要：针对常规红外干扰技术存在的能量无法集中、隐蔽性差且无法进行变倍切换等实际问题,提出一种离轴双反射式激光干扰扩束系统的设计方案,并对离轴双反射镜组,转向平面反射镜及支撑固定机构等主要组成部分进行了光机结构设计.为实现扩束比的变倍切换功能,采用新型离轴副镜组件设计;为减小镜面变形,离轴主副镜组均采用微应力设计.分析结果表明,在-20^+60℃温度范围内,主副镜组轴向最大位移小于等于0.01mm,主副镜组的反射镜面形误差小于等于71.9nm;系统一阶固有频率108.3Hz,其支撑结构应力响应远小于材料的屈服极限.实际测试发现,系统可实现1:10.02(19.92,25.02)扩束比,满足设计技术指标要求.分析及试验结果表明,系统光机结构设计合理,完全满足实际应用要求.

摘要：从现代防火安全观出发,对汗蒸房火灾危险性进行深入分析。从技术措施和管理措施两个方面入手,提出加强行业监管,出台汗蒸房消防技术标准,严格汗蒸房消防设计、装修材料、合理电气设计、建立微型消防站等措施。

摘要：结合半固态合金成分设计原则,通过热力学计算,研究了3种成分的半固态镁合金。通过组织观察和流变学参数分析表明,半固态组织的形成速度随铝含量增加而加快,固相粒子变得细小、圆整。分析得出铝元素主要通过两个方面影响半固态组织,一个是液相形核,另一个是再结晶晶粒尺寸。随着铝含量增加,液相形核数量增多,再结晶晶粒尺寸减小,这些都促进了半固态组织的形成和演变,有利于镁合金半固态加工。

摘要：设计了一种由内嵌金属方芯的金属-绝缘体-金属方形气腔以及两个侧耦合波导组成的耦合结构,并采用有限元方法研究了该结构的传播特性.结果表明:通过对气腔内金属方芯偏离角和偏离距离的调节可以获得并调制Fano共振;该Fano共振由对称破缺或几何效应影响左右波导和谐振腔之间耦合区域中的场分布强度所致,场分布模式的变化是由波导模和腔模之间的干涉引起的.此外,Fano共振的光谱位置和调制深度对偏差参数十分敏感,通过计算不同偏差角及偏差距离下的折射率传感特性发现,其折射率敏感度最高达1 508nm/RIU,品质因数最高达1 308.研究结果为设计更加灵活、简单、高效的片上等离子体纳米传感器提供了理论依据.

摘要：望东长江公路大桥主桥为主跨638m的双塔双索面组合梁斜拉桥,其上部结构采用工厂化、装配化的方案架设。为解决组合梁整体吊装施工时存在的桥面板开裂及梁段不匹配的问题,采用RM2006和ANSYS软件分别建立全桥及梁段局部有限元模型,对斜拉索分次超张退张法和防错台架设法进行研究,提出一种基于节段全过程状态(内力状态、几何状态)优化的上部结构装配化架设方法。结果表明:斜拉索分次超张退张法可优化节段施工全过程内力,解决了新梁段起吊对前序梁段引起的较大桥面板拉应力问题;通过斜拉索张拉与钢主梁工地连接工序的优化调整,改善了已架设梁段与待架设梁段匹配时的几何状态,保证了梁段匹配的可靠性。