基于微动调制的FMCW SAR无源压制干扰方法

调频连续波(FMCW)合成孔径雷达(SAR)体积小、重量轻、成本低、功耗低等优点,在无人机等小型飞行平台中具有较大的应用潜力,对FMCW SAR的干扰也将成为目前干扰技术研究的重点;在构建旋转微动目标回波模型的基础上,分析了FMCW SAR旋转微动目标的干扰特性,并进一步提出了一种基于微动调制的FMCW SAR无源压制干扰方法;该方法利用旋转角反射器在距离向和方位向上形成的二维干扰条带,能够实现对被掩护目标的有效保护;文章详细分析了对FMCW SAR实施干扰时旋转角反射器的参数选择方法,并利用仿真实验验证了理论分析与所提无源压制干扰方法的有效性。     

Novel pyrrolo[2,3-d]pyrimidine derivatives: Design,synthesis, structure elucidation and in vitro anti-BVDV activity

The progression of drug resistance of viral infection justifies the discovering of new anti-viral agents. Thus, a novel series of pyrrolopyrimidine derivatives 5–7 and 9–18 were designed, synthesized and fully characterized by IR, mass spectroscopy, NMR, and elemental analysis. The structure of 4,6-dichloro-pyrrolo[2,3-d]pyrimidine 10 elucidated by single crystal X-ray diffraction. Herein, we reported the first pyrrolo[2,3-d]pyrimidine compounds with trichloromethane at position 2 of the pyrimidine ring. As initial biological activity screening, evaluation of the pyrrolo[2,3-d]pyrimidine compounds as anti-BVDV (Bovine Viral Diarrhea Virus) was examined. The compounds 11, 13, 16 and 17 exhibited excellent activity as a potent inhibitor against BVDV. Structure activity relationship showed that the pyrrolo[2,3-d]pyrimidine molecules presenting hydrogen atom or trichloromethyl group on C2 and chlorine, sulfur, pyrrolidine or methoxy groups on C4 of the pyrimidine ring showed high activity as anti-BVDV in comparison with the compounds which have Cl or CH₃ on C2 position.     

Design,synthesis and antiproliferative activity against human cancer cell lines of novel benzo-, benzofuro-, azolo- and thieno-1,3-thiazinone resorcinol hybrids

In this paper we report the design and synthesis of novel derivatives of the 4H-3,1-benzothiazinone type and heterocyclic analogues, i.e. benzofuro-, azolo- and thieno-1,3-thiazin-4-ones possessing 2,4-dihydroxyphenyl substituent. The compounds were obtained by the one-step reaction of aminobenzamides or heterocyclic aminocarboxamides with aryl-modified sulfinylbis[(2,4-dihydroxyphenyl)methanethione]. Evaluation of their antiproliferative potency against human cancer cell lines showed that the activity of some analogues was similar to that of cisplatin. The highest activity and low toxicity were found for 6-tert-butyl-2-(5-chloro-2,4-dihydroxyphenyl)-4H-thieno[3,2-d][1,3]thiazin-4-one. The structure–activity elucidation reveals that the most active compounds are those with a thienothiazin-4-one and benzofuro[3,2-d][1,3]thiazin-4-one skeleton and the presence of the hydrophobic substituent (Et, Cl) in the benzenediol moiety increases their antiproliferative potency. The ADMET properties of selected compounds including metabolic stability and toxicity profile were estimated in silico.     

实时光电混合SA■数据处理器

设计了一种光电混合综合孔径雷达(SAR)数据处理器,它利用声光器件(AOD)作为实时输入电-光转换器,利用光学系统实现SAR数据距离维的聚焦,利用CCD完成SAR数据在方位维的压缩并同时输出处理后的SAR图像。给出了实验室实时完成SAR数据距离维聚焦的有关图片。     

磺酰脲除草剂分子与受体作用的初级模型

磺酰脲除草剂分子与受体作用的初级模型赖城明，袁满雪，李正名，贾国锋，王玲秀（南开大学元素有机化学国家重点实验室化学系，天津，３０００７１）（南开大学元素有机化学研究所）关键词磺酰脲分子，受体作用模型，构效关系磺酰脲类具有超高效除草性能。Ｓｃｈｌｏｓｓ...     

基于自校验直接线性变换的星载SAR图像定位方法研究

应用摄影测量理论,将星载SAR图像近似看作一个多中心投影传感器获取的等效影像,基于星载 SAR共线方程给出了SAR图像的自校验直接线性变换定位模型.选用一景北京地区RadarSat影像进行实验.结果表明,自校验直接线性变换模型表达简单,求解稳定,不需要任何轨道信息和成像参量且校正准确度保持在像素级范围之内,因而该模型适用于星载SAR图像的准确定位.     

Outliers in SAR and QSAR: Is unusual binding mode a possible source of outliers?

A lead optimization is usually carried out by structure-activity relationship (SAR) and/or quantitative structure-activity relationship (QSAR) studies. One of the assumptions in SAR and QSAR studies is that similar analogs bind to the same binding site in a similar binding mode. One often observes that there are outliers, especially in QSAR. However, most QSAR studies are carried out focusing their attention to the development of QSAR and leave the outliers without much attention. We searched a number of ligand-bound X-ray crystal structures from the protein structure database to find evidences that could indicate a possible source of outliers in SAR or QSAR. Our results show that unusual binding mode could be a source of outliers. Electronic supplementary material The online version of this article (doi:) contains supplementary material, which is available to authorized users.     

Recovering laboratory doses using fine-grained quartz from Chinese loess

Here we report the results of dose recovery experiments carried out on fine-grained quartz from a Holocene sample in Chinese loess. Optical bleaching prior to giving a 9.35 Gy dose in the laboratory was carried out using artificial light sources, namely blue light emitting diodes (LEDs) and a solar simulator, followed by more than 24 h storage at room temperature. Stimulating the quartz with blue LEDs at room temperature resulted in overestimation of the recovered dose, whereas using the same stimulation time at temperatures above 150 °C resulted in the correct value for the recovered dose. Exposure to the solar simulator for times less than 200 min resulted in overestimation of the dose, whereas progressive underestimation was found for longer bleaching times. When doses of up 5333 Gy were given ahead of a 200 min exposure to the solar simulator, the dose recovered depended upon the magnitude of the previous dose, thus questioning the general application of a simple dose recovery experiment.     

7-羟基异黄酮及其衍生物的合成与选择性雌激素受体结合的构效关系研究

以多酚类化合物和多取代苯乙酸类化合物为原料,用一锅法合成了24个7-羟基异黄酮类化合物;并从一锅法制得的3d,3g经脱除甲基得到两个2'-羟基取代的异黄酮化合物4a和4b.雌激素受体(Estrogen receptors,ERs)的选择性结合活性试验表明:26个化合物(包括4个新化合物3r,3s,3u和3v)中,9个化合物与ERβ相对于ERα的选择性作用强于染料木素(Genistein);发现7,8-二羟基异黄酮类化合物与ERβ相对结合能力高于相应7-羟基异黄酮类化合物;4'取代基对化合物与ERβ结合相对于ERα的选择性影响从大到小为:H>Cl>F>OH;2',3'及5'位取代基降低异黄酮对ERα和ERβ的亲和性.     

The Application of Structure-Activity Relationships (SARs) in the Aquatic Toxicity Evaluation of Discrete Organic Chemicals

Abstract

The Office of Pollution Prevention and Toxics (OPPT), United States Environmental Protection Agency (USEPA) routinely uses structure-activity relationships (SAR) for the aquatic hazard assessment of new chemicals submitted under Section 5 of the Toxic Substances Control Act (TSCA). With 15 years of experience and the general acceptance of toxicity predictions based on SARs, OPPT has expanded the use and application of the methodology to include existing chemicals used in printing, dry cleaning, and paint stripping. SAR analysis has also been used in the hazard evaluation of the U.S. and EU/OECD high production volume (HPV) chemicals. This paper describes the assumptions, limitations, and methodology for the use of SARs to evaluate large sets of discrete organic chemicals.