激活型有机光声造影剂的应用

光声(PA)成像作为一种结合了光学和声学成像优势的新型成像方式,具有深层组织穿透和高空间分辨率等优点,在重大疾病的早期影像诊断方面有着巨大的应用前景.然而传统的PA造影剂依然存在信噪比低、选择性及特异性差等不足,容易产生假阳性诊断结果.激活型PA造影剂可以有效的降低背景噪声,并提升成像的灵敏度和特异性,是目前PA造影剂...     

The reaction of allyldialkyltelluronium bromides with anilines

Allyldialkyltelluronium bromides were treated with aromatic amines in 1,2-dichloroethane, readily giving allyl aryl amines in excellent yields.     

Synthesis of fluorinated monomers through sulfinatodehalogenation and related reactions

Using sulfinatodehalogenation and related reagent systems several groups of perfluoroalkylated compounds including olefins, dienes, phenolic compounds and aromatic dicarboxylic acids were synthesized which may be useful as potential monomers.     

X射线荧光分析中X射线管原级能谱分布的测定

确切知道X射线管激发的原级能谱分布是X射线荧光分析中的一个重要前提,所用能谱分布函数的准确度大大影响了最终的测量结果。提出利用间接测量法,选用合适的参量模型来描述X射线的原级能谱分布。依靠实验测得的厚靶纯元素样品的荧光强度,利用已知的理论公式,建立非线性方程,优化得到参量模型中的参量值。通过比较实验测得的元素的荧光强度值和利用得到的能谱分布函数计算的理论值,证明此种方法是可行的。     

光纤拉曼放大器中增益的偏振相关特性研究

提出了一种改进的、可用于计算偏振相关拉曼增益的光纤拉曼放大器的非线性耦合波方程。建立了单模双折射光纤拉曼增益的数学模型,分析了线偏振抽运光以与光纤快轴成45°激励的单模双折射光纤拉曼放大器模型与实际具有随机双折射的光纤拉曼放大器的拉曼增益偏振相关特性的等价性。基于上述模型,提出了一个可定量表征单模光纤偏振模色散统计特性的拉曼增益偏振相关因子,用以替代常规的光纤拉曼放大器非线性耦合波方程中的偏振相关因子。计算结果与已报道文献的实验数据非常吻合。同时对抽运增益在同向和反向抽运方式下截然不同的增益偏振相关特性给出了合理的解释。     

Flowfield of a helicopter submerged inlet with power output shaft

The submerged inlet is an attractive configuration for advanced helicopters due to its high stealth performance and low external drag.In this paper,a submerged ...     

How the Aggregates Determine Bound Rubber Models in Silicone Rubber? A Contrast Matching Neutron Scattering Study

The correlation between aggregates and bound rubber structures in silicone rubbers(S(phr)) with various silica fractions(ΦSi) has been investigated by contrast matching small-angle neutron scattering(SANS), swelling kinetics, and low-field nuclear magnetic resonance(NMR).Mixed solvents with deuterated cyclohexane fractions of 4.9% and 53.7% were chosen to match the scattering length densities of the matrix(SMP(phr)) and the filler(SMS(phr)), respectively. All the data consistently suggest that:(i) There is a critical threshold ΦSic between 10 and 30 phr;below ΦSic, the isolated aggregates are dominant, while beyond ΦSic, some rubber fraction is trapped among the agglomerate;(ii) ΦSiindependent thicknesses around 7.5 nm(NMR) and 8.6 nm(SANS) suggest that the bound rubber formation is determined by inherent properties of the components, and the power-law around 4.2 suggests an exponential changed gradient density of the bound rubber;(iii) SMS(80) presents a bicontinuous bound rubber with three characteristic lengths of 41, 100, and 234 nm. The expanded correlation length, a 20 nm smaller aggregate sizes suggest that such existent bicontinuous network in dry samples with less ΦSi is kind of impacted by swelling. With the obtained bound rubber models, the reinforcing mechanism of filled silicone rubber is elucidated.     

Tributylstibine-mediated olefination of carbonyl compounds with bromomalonic ester and with dibromomalonic ester—A possible pathway through a stibonium ylide via halophilic initiation by tertiary stibines

Tributylstibine can mediate the olefination of carbonyl compounds with bromomalonic ester and with dibromomalonic ester. An initial halophilic attack of tributylstibine on the bromine of bromomalonic or dibromomalonic ester forming an ion pair of bromotributylstibonium cation and malonic (A) or bromomalonic ester carbanion (B) , respectively, is proposed. These ion pairs react with carbonyl compounds to achieve subsequent olefination. Alternatively, 2 equiv of A collapse, with elimination of malonic ester, to form stiborane D , and the ion pair B reacts with another equivalent of tributylstibine to form stiborane D. This last undergoes a Wittig-type reaction with carbonyl compound to achieve olefination.     

Newly Emerging Strategies in Antiviral Drug Discovery: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Anniversary

Viral infections pose a persistent threat to human health. The relentless epidemic of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become a global health problem, with millions of infections and fatalities so far. Traditional approaches such as random screening and optimization of lead compounds by organic synthesis have become extremely resource- and time-consuming. Various modern innovative methods or integrated paradigms are now being applied to drug discovery for significant resistance in order to simplify the drug process. This review provides an overview of newly emerging antiviral strategies, including proteolysis targeting chimera (PROTAC), ribonuclease targeting chimera (RIBOTAC), targeted covalent inhibitors, topology-matching design and antiviral drug delivery system. This article is dedicated to Prof. Dr. Erik De Clercq, an internationally renowned expert in the antiviral drug research field, on the occasion of his 80th anniversary.     

The System Profile of Renal Drug Transporters in Tubulointerstitial Fibrosis Model and Consequent Effect on Pharmacokinetics

With the widespread clinical use of drug combinations, the incidence of drug–drug interactions (DDI) has significantly increased, accompanied by a variety of adverse reactions. Drug transporters play an important role in the development of DDI by affecting the elimination process of drugs in vivo, especially in the pathological state. Tubulointerstitial fibrosis (TIF) is an inevitable pathway in the progression of chronic kidney disease (CKD) to end-stage renal disease. Here, the dynamic expression changes of eleven drug transporters in TIF kidney have been systematically investigated. Among them, the mRNA expressions of Oat1, Oat2, Oct1, Oct2, Oatp4C1 and Mate1 were down-regulated, while Oat3, Mrp2, Mrp4, Mdr1-α, Bcrp were up-regulated. Pearson correlation analysis was used to analyze the correlation between transporters and Creatinine (Cr), OCT2 and MATE1 showed a strong negative correlation with Cr. In contrast, Mdr1-α exhibited a strong positive correlation with Cr. In addition, the pharmacokinetics of cimetidine, ganciclovir, and digoxin, which were the classical substrates for OCT2, MATE1 and P-glycoprotein (P-gp), respectively, have been studied. These results reveal that changes in serum creatinine can indicate changes in drug transporters in the kidney, and thus affect the pharmacokinetics of its substrates, providing useful information for clinical use.