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991.
Bi Liu Gang‐Qiang Wang Yan‐Hong Peng Xiu‐Qin Tang Guo‐Wen Hu 《Journal of heterocyclic chemistry》2019,56(12):3423-3428
In this work, a series of butylene tethered heteronuclear 7‐fluoroisatin‐isatin scaffolds 4a to 4h were designed and synthesized, and the antimycobacterial activity profiles, cytotoxicity together with inhibitory activity against MTB DNA gyrase, were also investigated. All the synthesized heteronuclear scaffolds were active against MTB H37Rv and MDR‐MTB strains, and some of them were more potent than isoniazid ( INH ), rifampicin ( RIF ), ethambutol ( EMB ) against MDR‐MTB strain. The structure‐activity relationship demonstrated that the substituents on C‐3 position of 7‐fluoroisatin and isatin moieties were closely related with the activity, and hydrogen bond donors were favorable to the activity. Scaffolds with different substituents showed higher activity than the analogs with the same substituents at this position of the two isatin motifs, which may be attributed to the synergistic effect. Among them, the most active scaffold 4e (MIC: 1 and 4 μg/mL) was comparable with the first‐line anti‐TB agent EMB against MTB H37Rv, and ≥16‐fold more potent than INH , RIF , and EMB against MDR‐MTB strain, demonstrating its potential for fighting against infections caused by both drug‐sensitive and MDR MTB strains. Moreover, scaffold 4e also possessed excellent toxicological profiles and promising inhibitory activity against MTB DNA gyrase. Thus, scaffold 4e could act as an ideal platform for further optimization. 相似文献
992.
THE EIGENVALUE PERTURBATION BOUND FOR ARBITRARY MATRICES 总被引:1,自引:0,他引:1
Wen Li Jian-xin Chen 《计算数学(英文版)》2006,24(2):141-148
In this paper we present some new absolute and relative perturbation bounds for theeigenvalue for arbitrary matrices, which improves some recent results. The eigenvalueinclusion region is also discussed. 相似文献
993.
Palladium‐Catalyzed One‐Pot Three‐ or Four‐Component Coupling of Aryl Iodides,Alkynes, and Amines through CN Bond Cleavage: Efficient Synthesis of Indole Derivatives 下载免费PDF全文
Wei Hao Weizhi Geng Prof. Dr. Wen‐Xiong Zhang Prof. Dr. Zhenfeng Xi 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(9):2605-2612
An efficient synthesis of N‐substituted indole derivatives was realized by combining the Pd‐catalyzed one‐pot multicomponent coupling approach with cleavage of the C(sp3)?N bonds. Three or four components of aryl iodides, alkynes, and amines were involved in this coupling process. The cyclopentadiene–phosphine ligand showed high efficiency. A variety of aryl iodides, including cyclic and acyclic tertiary amino aryl iodides, and substituted 1‐bromo‐2‐iodobenzene derivatives could be used. Both symmetric and unsymmetric alkynes substituted with alkyl, aryl, or trimethylsilyl groups could be applied. Cyclic secondary amines such as piperidine, morpholine, 4‐methylpiperidine, 1‐methylpiperazine, 2‐methylpiperidine, and acyclic amines including secondary and primary amines all showed good reactivity. Further application of the resulting indole derivatives was demonstrated by the synthesis of benzosilolo[2,3‐b]indole. 相似文献
994.
改性Y分子筛的酸碱性能及吸附性能的研究 总被引:2,自引:1,他引:2
吡啶、吡咯、苯、甲苯、乙苯作为探针分子,在Li+, Na+, K+, Cs+改性的Y型分子筛上进行吸附,用TPD及IR方法系统地研究了不同碱金属离子改性的Y型分子筛的酸碱性能和吸附性能的变化. 结果表明,按Li、Na、K、Cs的顺序, 随着碱金属离子半径的增大, 其L酸酸强度依次减弱,L碱的强度逐渐增强.由于改性Y型分子筛所含碱金属离子的不同,其对芳烃的吸附的强弱及吸附量的大小亦不同.随着骨架外的阳离子的半径逐渐增大,碱的强度逐渐增强,与芳烃的作用愈强烈,导致TPD脱附峰温增高及芳烃和侧链上的C-H伸缩振动谱带向低波数位移愈多.由于位阻的原因,对含同一种碱金属离子的分子筛来说,随着芳烃侧链C数的增加,芳烃的吸附量逐渐减小. 相似文献
995.
高效液相色谱串联质谱测定蜂蜜、蜂王浆中氯霉素残留 总被引:7,自引:0,他引:7
前处理方法包括添加同位素内标氯霉素-d5和采用10%偏磷酸沉淀蜂王浆产品中的蛋白质,上清液经乙酸乙酯提取,自制硅胶柱和Oasis小柱净化。净化后的提取溶液用高效液相色谱-电喷雾电离质谱检测,多反应监测3对离子(321.0/256.9、321.0/194.0、321.0/175.8)。该方法对不同基质样品的加标回收率为91%-107%;相对标准偏差小于10%;蜂蜜和蜂王浆的方法检出限分别为0.1μg/kg和0.2μg/kg。 相似文献
996.
Micron-sized hollow silica spheres whose shells are made up of mesocellular silica foams(MCFs) have been synthesized by one-pot sol-gel method in benzene/water/P123 emulsion.The material is characterized with SEM,TEM,BET and ~(29)Si MAS NMR. The results show that the MCFs of the unique shell of hollow silica spheres were connected by large windows with a narrow distribution of~10 nm in diameter,the inner space of the hollow sphere is accessible.And the formation mechanism of the hollow silica spheres is ... 相似文献
997.
Wang Y Ding Y Wen H Lin Y Hu Y Zhang Y Xia Q Lin Z 《Combinatorial chemistry & high throughput screening》2012,15(4):347-353
Drug resistance to existing antibiotics poses alarming threats to global public health, which inspires heightened interests in searching for new antibiotics, including antimicrobial peptides (AMPs). Accurate prediction of antibacterial activities of AMPs may expedite novel AMP design and reduce the costs and efforts involved in laboratory screening. In the present study, a novel quantitative prediction method of AMP was established by quantitative structure-activity relationship (QSAR) modeling based on the physicochemical properties of amino acids. The indices of these physicochemical properties were used to define AMP. The structural variables were optimized by stepwise regression (STR). Three series of AMPs from the QSAR model were constructed by multiple linear regressions (MLR). These QSAR models showed good performance in reliability and predictability. The normalized regression coefficients of the QSAR model and the contribution of amino acids at each position of AMP may determine the suitableness of a particular residue at any given position. QSAR models constructed by STR-MLR should prove to be useful tools in peptide design with respect to the calculation, explanation, good and reliable performance, and definition of physiochemical properties. 相似文献
998.
Control of N‐Heterocyclic Carbene Catalyzed Reactions of Enals: Asymmetric Synthesis of Oxindole‐γ‐Amino Acid Derivatives 下载免费PDF全文
Dr. Xiang‐Yu Chen Jia‐Wen Xiong Qiang Liu Sun Li He Sheng Dr. Carolina von Essen Prof. Dr. Kari Rissanen Prof. Dr. Dieter Enders 《Angewandte Chemie (International ed. in English)》2018,57(1):300-304
A strategy to control the switch between a non‐cycloaddition reaction and a cycloaddition reaction of enals, using N‐heterocyclic carbene (NHC) catalyisis, has been developed. The new scalable protocol leads to γ‐amino‐acid esters bearing a tetrasubstituted stereocenter in good yields and high stereoselectivities by homo‐Mannich reactions of enals and isatin‐derived ketimines. By simply changing the N‐ketimine substituent to an ortho‐hydroxy phenyl group, the corresponding spirocyclic oxindolo‐γ‐lactams are obtained. 相似文献
999.
1000.
A Novel Dihydroflavone from the Roots of Uvaria Macrophylla 总被引:1,自引:0,他引:1
A new dihydroflavone (1), named macrophyllol A, was isolated from the roots of Uvaria macrophylla. Its structure was elucidated on the basis of spectroscopic evidence. 相似文献