Het(aryl)isatin to het(aryl)aminoindoline scaffold hopping: A route to selective inhibitors of matrix metalloproteinases

Matrix metalloproteinases (MMPs) are a large family of zinc-dependent endoproteases known to exert multiple regulatory roles in tumor progression. A variety of chemical classes have been explored for targeting individual MMP isoforms. In the present study, we further developed our isatin based scaffold BB0223107 capable of binding to and inactivating MMP-2 in a zinc-independent manner (Agamennone et al., 2016). Forty four new compounds were synthesized based on the modified BB0223107. All compounds were tested in enzyme inhibition assays against MMP-2, ?8 and ?13. SAR studies demonstrated that 5-het(aryl)-3-aminoindolin-2-ones (37–39) were active toward MMP-2 and MMP-13. The most potent compounds 33 and 37 displayed an IC₅₀ of 3 µM against MMP-13 and showed a negligible activity toward MMP-8; almost all new compounds were inactive toward MMP-8. Replacement of the isatin ring with a biaryl system (compound 33) did not decrease the potency against MMP-13 but reduced the selectivity. Structure-based computational studies were carried out to rationalize the inhibitory activity data. The analysis of binding geometries confirmed that all fragments occupied the S1′ site in the three enzymes while no ligand was able to bind the catalytic zinc ion. To the best of our knowledge, this is the first example of 3-aminoindolin-2-one-based MMP inhibitors that, based on the computer modeling study, do not coordinate the zinc ion. Thus, the het(aryl)-3-aminoindolin-2-one derivatives emerge as a drug-like and promising chemotype that, along with the hetaryl variations, represents an alternative and thrifty tool for chemical space exploration aimed at MMP inhibitor design.     

A self-penetrating and chemically stable zinc (ii)-organic framework as multi-responsive chemo-sensor to detect pesticide and antibiotics in water

Guided by the self-penetrating features can improve the stability of metal organic frameworks (MOFs), an unprecedented 3D self-penetrated framework, {[Zn (tptc)_0.5(bimb)]·H₂O}_n ( NUC-6 , here NUC corresponding to North University of China), with 3D (4,4)-c {8⁶} net, was designed. Benefit from the high chemical stability and excellent luminescent property, NUC-6 can be act as an efficient multi-response chemo-sensor in detecting dichloronitroaniline pesticide and nitrofuran antibiotics in water with the detection limits are 116 ppb for DCN pesticide, 16 ppb for NFT antibiotic, and 12 ppb for NTZ antibiotic. Besides, the mechanisms of luminescence quenching were revealed from the viewpoint of internal filter effect (IFE) and photo-induced electron transfer (PET), implied by the optical spectroscopy and quantum chemical calculation. This work provides a promising strategy to design stable MOFs by improving the self-penetrating features and to expand their practical applications in the detection of organic pollutants in aqueous medium.     

FTIR光谱遥测红外药剂的燃烧温度

本文利用遥感FTIR光谱，对红外药剂的燃烧特性进行了研究。在分辨率为4cm^-1时，收集4700－740cm^-1波段的光谱。从HF等燃烧产物发射的分子振转基带精细结构的谱线强度分布，可以对燃烧温度进行遥感测定，并给出了燃烧温度随时间的变化关系，实验结果表明燃烧表面附近温度梯度很大，存在着急剧的变化温度场，同时也说明，在不干扰火焰温度场的情况下，利用遥感FTIR光谱对剧烈的、非稳态快速燃烧的火焰温度进行连续实时的遥感测量，是一种快速、准确、灵敏度高的测温方法，显示了它在燃烧温度测量、产物浓度测试以及燃烧机理研究等方面的应用前景。     

激光雷达中层大气遥感技术

介绍了中科院武汉物理与数学研究所瑞利激光雷达的技术特点，并从其对武汉地区中层大气密度和温度廓线探测的典型结果，给出了该激光雷达对中层大气主要参数的探测能力。     

Long-wavelength GaInAsSb/AlGaAsSb DFB lasers emitting near 2.6 μm

We have successfully fabricated and characterized room temperature continuous wave (cw) GaInAsSb/AlGaAsSb distributed feedback lasers emitting in the wavelength region between 2.499 and 2.573 μm. To the best of our knowledge, this is the longest emission wavelength realized with a GaSb-based DFB laser diode. The laser structure used for DFB processing was grown by solid source molecular beam epitaxy. A DFB concept requiring no subsequent overgrowth step was used by defining first-order Cr-Bragg gratings laterally patterned to a ridge waveguide. Threshold currents smaller than 60 mA and room temperature cw output powers up to 6.5 mW were obtained. The laser diodes show single mode emission with side mode suppression ratios (SMSR) of up to 32 dB.     

遥感傅里叶变换红外光谱的大气层析技术

遥感傅里叶变换红外光谱层析技术是一项新的气体分析技术，它可用于构造气体浓度峰图形，定量分析工业污染气体总释放量等方面，随着算法的不断优化，在重构气体在空间的分布方面，遥感傅里叶变换红外光谱层析技术正在不断成长。     

Iterative regularization methods for atmospheric remote sensing

In this paper we present different inversion algorithms for nonlinear ill-posed problems arising in atmosphere remote sensing. The proposed methods are Landweber's method (LwM), the iteratively regularized Gauss-Newton method, and the conventional and regularizing Levenberg-Marquardt method. In addition, some accelerated LwMs and a technique for smoothing the Levenberg-Marquardt solution are proposed. The numerical performance of the methods is studied by means of simulations. Results are presented for an inverse problem in atmospheric remote sensing, i.e., temperature sounding with an airborne uplooking high-resolution far-infrared spectrometer.     

斐索梯度折射率光纤透镜传感实验

采用LD泵浦的单纵模Nd：YVO4倍频激光器、梯度折射率光纤透镜等器件构成斐索梯度折射率光纤透镜传感实验仪．本文介绍了实验装置和实验原理，并给出了实验结果。     

New stereoselective synthesis of the peptidic aminopeptidase inhibitors bestatin, phebestin and probestin

Peptidic aminopeptidase inhibitors, bestatin, phebestin and probestin have been prepared by stereo- and regiocontrolled reactions from a common α,β-epoxy ester precursor.     

A new approach towards peptidosulfonamides: synthesis of potential inhibitors of bacterial peptidoglycan biosynthesis enzymes MurD and MurE

Peptidosulfonamides are an emerging group of peptidomimetics with a variety of applications in medicinal chemistry. We present a novel approach to the synthesis of peptidosulfonamides, and apply it to a series of new potential inhibitors of the bacterial peptidoglycan biosynthesis enzymes MurD and MurE. The synthesis was conducted via N-phthalimido β-aminoethanesulfonyl chlorides, which are new building blocks for the synthesis of peptidosulfonamides. In the most crucial step, sulfonic acids or their sodium salts were converted into the corresponding sulfonyl chlorides using an excess of either SOCl₂ or SOCl₂/DMF, and then coupled to the C-protected amino acid. None of the compounds significantly inhibited MurD, however, some inhibited MurE; one had an IC₅₀ below 200 μM, which constitutes a promising starting point for further development. Molecular modelling simulations were performed on two analogues to investigate the absence of inhibitory activity of the sulfonamide compounds on MurD.