摘要:
In high-throughput screening, the immobilization of bio-target shows a significant effect on the target performance, especially the conformation. This, ultimately, has an influence on the screening quality. In present article, a series of mathematical and physical models for target immobilization were established. As shown, in the immobilization process, if the plot of C*/Q versus C* is a straight-line, the drugs obtained from in vitro screening are probably applicable to in vivo environment. Otherwise, when the linearity exists between ln Q or Q and ln C*, particularly between Q and ln C*, additional competition-experiments of known ligands are necessary. In addition, the immobilization in multilayer form, as well as its impact on screening quality, was also discussed in this article (C*, the equilibrium concentration of bio-target; Q, the adsorbance).
作者:
Zu-ming Liu;Chang-jian Hou;Hai-yang Tu;Guang-fu Yang
作者机构:
[Zu-ming Liu; Chang-jian Hou; Hai-yang Tu; Guang-fu Yang] Key Laboratory of Pesticide & Chemical Biology,Ministry of Education;[Zu-ming Liu; Chang-jian Hou; Hai-yang Tu; Guang-fu Yang] College of Chemistry,Central China Normal University,Wuhan 430079 China
会议名称:
International Conference on Molecular Machines and Sensors(2007年分子机器和分子探针国际会议)
会议时间:
2007-5-7
会议地点:
上海
会议主办单位:
华东理工大学
会议论文集名称:
International Conference on Molecular Machines and Sensors(2007年分子机器和分子探针国际会议)论文集
摘要:
5,5-Dimethyl-1,3,2-dioxa phosphorocyclohexane 2-phosphoryl thioureas (4a-I) were synthesized by the reaction of phosphorus oxychloride with 2,2-dimethylpropanediol, potassium isothiocyanate, and substituted arylamines successively. IR, H-1-NMR and elementary analysis characterized their structures. The antibacterial test showed they were efficient against Fusarium oxysporium and Rhizatonia solani.
摘要:
A simple strategy for the design of an electrochemical sensor based on enzyme-induced growth of gold nanoparticles (AuNPs) without adding gold nano-seeds was proposed with acetylcholinesterase (AChE) as a model. Owing to the excellent biocompatibility of chitosan film for the subsequent assembly of biological molecules, chitosan film was first electrochemically deposited on Au electrode surface from a mildly acidic chitosan solution via a negative voltage bias. Based on immobilization of AChE, a stable AChE sensor (AChE-CS/Au) was constructed. The immobilized AChE mediated hydrolysis of ATCl and yielded a reducing agent thiocholine. In the presence of AuCl4-, AuNPs were formed without addition of any metal nanoparticles. Atomic force microscopy (AFM) images proved that small spherical nanoparticles could grow on the enzyme-modified surface after incubation in HAuCl4 and ATCl solution. [Fe(CN)(6)](3-/4-) redox system was used as a probe to indicate the process of electron transfer across the interface and also analyze the enzyme inhibitor quantitatively. The inhibition of malathion on AChE was proportional to its concentration in the range of 0.1-500 ng ml(-1) (R= 0.9989), with detection limit of 0.03 ng ml(-1). (c) 2007 Elsevier B.V All rights reserved.
作者机构:
[Li, Liang; Xiao, Wen-Jing; Chen, Jia-Rong; Liu, Xiao-Peng; Qiao, Yong-Feng; Zhang, Jian-Ming; Zhu, Xiao-Yu] Cent China Normal Univ, Coll Chem, Minist Educ Res, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Xiao, Wen-Jing] Cent China Normal Univ, Coll Chem, Minist Educ Res, Key Lab Pesticide & Chem Biol, 152 Luoyu Rd, Wuhan 430079, Peoples R China.
通讯机构:
[Xiao, Wen-Jing] C;Cent China Normal Univ, Coll Chem, Minist Educ Res, Key Lab Pesticide & Chem Biol, 152 Luoyu Rd, Wuhan 430079, Peoples R China.
摘要:
An efficient asymmetric aldol condensation of ketones with isatins has been developed using an L-proline-derived bifunctional organocatalyst. This strategy allows the enantioselective synthesis of a variety of 3-alkyl-3-hydroxyindolin-2-ones with a stereogenic quaternary carbon center in excellent yields with good to excellent enantiomeric excess. The method has been applied to the enatioselective synthesis of (S)-convolutamydine successfully. (c) 2007 Elsevier Ltd. All rights reserved.
作者机构:
Univ Ottawa, Dept Chem, Ctr Catalysis Res & Innovat, Ottawa, ON K1N 6N5, Canada.;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Hubei, Peoples R China.;[Yang, Qian] Univ Ottawa, Dept Chem, Ctr Catalysis Res & Innovat, 10 Marie Curie, Ottawa, ON K1N 6N5, Canada.
通讯机构:
[Yang, Qian] U;Univ Ottawa, Dept Chem, Ctr Catalysis Res & Innovat, 10 Marie Curie, Ottawa, ON K1N 6N5, Canada.
摘要:
A series of new pyrrolidine derivatives were prepared directly in very good yields, from the substrates containing a basic or nucleophilic N atom via ring-closing enyne metathesis reaction under mild reaction conditions. Moreover, the reaction occurs smoothly without the presence of ethylene gas.
作者机构:
[Xinyong Li; Weiwei Jin; Caibao Chen; Wen-Jing Xiao] Key Laboratory of Pesticide and Chemical Biology,Ministry of Education,College ot Chemistry,Central China Normal University,152 Luoyu Road,Wuhan,Hubei 430079,China
会议名称:
第17届国际磷化学学术会议(The 17th International Conference on Phosphorus Chemistry)
会议时间:
2007-4-15
会议地点:
厦门
会议主办单位:
中国化学会
会议论文集名称:
第17届国际磷化学学术会议(The 17th International Conference on Phosphorus Chemistry)论文集
摘要:
A systematic work on the homo-pinacol coupling reactions of benzophenones, aldehydes, and acetophenones in aqueous media with InCl3/Al is described for the first time, in which various 1,2-diols are obtained in moderate to good yields. (c) 2006 Elsevier Ltd. All rights reserved.
摘要:
A pair of novel fluorescent molecular clips was synthesized from diethoxycarbonal glycoluril cyclic ether and 1,2-dihydroindazol-3-one. Their structures and conformations were confirmed by single crystal X-ray diffraction and chemosensory properties were studied by fluorescent spectroscope. Both of them exhibited selective recognition toward Fe3+ over other metal ions examined in DMF/CH3OH (50:1, v/v). (c) 2007 Elsevier Ltd. All rights reserved.