Current perspectives on benzoflavone analogues with potent biological activities: A review

Medicinal chemistry investigators have isolated and synthesized benzoflavone analogues with diverse bioactivities including enzyme inhibitory activity, central nervous system (CNS) activity, anti-inflammatory activity, anti-microorganism activity, hypoglycemic activity, and receptor modulating potential. SAR (Structure-Activity Relationship) studies have been conducted extensively and plenty of benzoflavone analogues have been prepared for potential targets. Herein, we review the pharmacology properties and SAR for benzoflavone analogues, and provide a brief summarization of synthetic strategies, wishing to give perspective on the research and development of benzoflavone derivatives.     

合成孔径雷达极化成像解译识别技术的进展与展望

极化合成孔径雷达(SAR)能够获取目标的全极化信息,在对地观测、灾害评估、侦察监视等民用和军用领域得到广泛应用。国内主要高校、中科院、工业部门和用户单位在该领域开展了卓有成效的工作,取得一大批标志性研究成果。该文简要综述了极化SAR成像解译识别领域的主要研究进展。在解译层面,主要介绍了极化目标分解和极化旋转域解译等理论方法的研究进展。在应用层面,结合研究团队的工作,探讨了上述理论方法在舰船检测、地物分类和建筑物损毁评估等领域的应用成效。最后,对极化SAR目标解译识别技术的研究进行了展望。      

一种星载SAR 电缆网EMC 设计与分析*

结合某型号海洋监测星载SAR 工程设计背景,首先阐述了星载SAR 应用特点及其对电缆网EMC 设 计的牵引需求,然后着重探讨了星载SAR 电缆网内涵及其EMC 设计规则,进而选取整星电缆网单机关重件———用 于波束控制的电缆组件,介绍了其EMC 设计过程,并通过Ansoft、SIWAVE、Q3D 等软件创建驱动端、负载端以及用于 互联的电缆组件电路模型,提取相应S 参数,对整个链路信号传输特性进行分析,最后进行了实测,实测结果与仿真 分析结果一致,验证了该电缆组件EMC 仿真设计有效。     

职业对讲机台站减少头部SAR测试的注意事项

本文提供了对讲机台站减少SAR测试的指导,文中提供的程序是基于对制造商和测试实验室如何测试对讲机台站和相关配件的测试调查而制定的.职业对讲机台站使用通常有多个天线、电池、身体佩戴和音频配件,一些台站大量多种多样的配件使SAR测试配置的数量也变得非常多,测试结果也是成千上万的组合.     

Design,Synthesis, Biological Evaluation and SARs of Novel N‐Substituted Sulfoximines as Potential Ryanodine Receptor Modulators

The sulfoximine group has been evaluated as a pharmacophore. Introducing the sulfoximine structure into medicinal compounds as exciting motifs has brought opportunities in drug discovery. In order to develop new ryanodine receptor (RyR) modulators, a series of phthalamides containing sulfoximine derivatives were designed, synthesized, and evaluated against oriental armyworm and diamondback moth for their insecticidal activities. These studies helped to elucidate the electronic and structural requirements around the sulfoximine motif for insecticidal activity. All new structures were synthesized and characterized by ¹H NMR, ¹³C NMR, HRMS and bioassay and a preliminary structure − activity relationship (SAR) was discussed. The biological assessment indicated that most title compounds showed good to excellent larvicidal activities. Compounds Ia , Ie , and If gave excellent insecticidal activity against oriental armyworm, which showed 100% larvicidal activity at 0.5 mg/L. All compounds showed 100% larvicidal activity at 0.1 mg/L against diamondback moth. In particular, the larvicidal activities of Ie , If , and Ih at 0.0001 mg/L were 50%, 20%, and 40%, respectively, reaching an activity as high as that of the commercial flubendiamide (40%, 0.0001 mg/L). Therefore, Ia , Ie , If and Ih could be considered as new lead structures for the development of new ryanodine receptor (RyR) modulators.     

6,7-二氧代-4-芳胺香豆素的设计、合成及分子对接研究

茶酚-氧位-甲基转移(COMT)酶抑制剂在治疗帕金森病中起到重要作用.通过对现有COMT酶抑制剂托卡朋和恩托卡朋结构与活性关系分析,推断含有儿茶酚结构的香豆素类化合物可能具有潜在的COMT酶抑制活性,因此设计合成了一类新型的6,7-二氧代-4-芳胺香豆素,通过理论计算,研究了此类化合物对COMT酶抑制活性.结果表明,设计的10种6,7-二氧代-4-芳胺香豆素与COMT酶的对接效果均较好,其中具有甲氧基乙基保护的儿茶酚结构化合物6,7-二[2-(甲氧基)乙氧]-4-(苯胺)香豆素(6b4)和6,7-二[2-(甲氧基)乙氧]-4-[(3-乙炔基)苯胺]香豆素(6b5)与COMT酶的对接效果尤为显著.     

A Wide-Band Approach to the Absolute Phase Retrieval in SAR Interferometry

Because of possible multiple solutions allowed, the unwrapping of interferometric fringe patterns in the spatial domain is an ill-posed problem which needs some a priori knowledge of the ground morphology for the solution of ambiguities. This is especially true for interferometric SAR (Synthetic Aperture Radar) data. In this paper we propose a different approach to InSAR processing for retrieving the height of ground points independently from each other, unlike most conventional phase unwrapping procedures, which operate in the spatial domain. The basic idea is to repeat raw data focusing by using range sub-bands centered at different frequencies, in order to find a point history of the interferometric phase variation vs. frequency. We introduce the general framework of the method together with considerations on the theoretical limits of applicability, then we report results of our simulations related to a wide-band SAR system. We show that, under certain conditions, height values can be retrieved over a network of coherent and strong scatterers, even when enclosed into low-coherence areas.     

图像域正则化特征增强SAR成像方法

通过分析SAR成像过程和正则化特征增强方法的特点，提出了一种在图像域进行正则化特征增强的成像方法。实验结果表明，本文方法能较好地抑制旁瓣和噪声，提高SAR图像的对比度，保护目标并提高图像的分辨率，且计算量比传统方法大大减小，有效提高了计算效率。     

基于正则化增强的SAR图像分割方法

SAR图像存在强烈的相干斑噪声,因此对SRN图像的分割非常困难。本文利用图像幅度的二维微分作为正则化约束对SAR图像进行增强,在抑制噪声的同时,保持了区域的边缘。对正则化增强的SAR图像进行简单的灰度门限分割,就可以取得很好的效果。试验结果表明了该方法的有效性。