除草剂抗性的分子机制研究
作者机构：
[杨光富; 朱晓磊; 郝格非; 戢风琴] 华中师范大学化学学院农药与化学生物学教育部重点实验室
会议名称：
中国化学会第26届学术年会化学生物分会场
会议时间：
2008-07
会议地点：
中国天津
关键词：
除草剂;抗性;分子机制;分子模拟
摘要：
<正>除草剂在杂草防治方面发挥了重要作用。但由于长期使用,杂草对除草剂的抗药性问题已经成为当前杂草防治中一个最严重的问题。从分子水平探讨除草剂抗性的分子机制对于合理使用除草剂、延缓现有除草剂抗性发生以及设计反抗性除草剂无疑具有重要的理论与实际意义。本论文采用分子
语种：
中文
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Synthesis and oxidation-induced DNA cross-linking capabilities of bis(catechol) quaternary ammonium derivatives
作者：
Song, Zhibin;Weng, Xiaocheng;Weng, Liwei;Huang, Jing;Wang, Xiaolin;...
期刊：
CHEMISTRY-A EUROPEAN JOURNAL ,2008年14(19):5751-5754 ISSN：0947-6539
通讯作者：
Zhou, Xiang
作者机构：
[Zhou, Yangyang; Weng, Liwei; Song, Zhibin; Huang, Jing; Wang, Xiaolin; Zhou, Xiang; Bai, Minghui; Weng, Xiaocheng] Wuhan Univ, Coll Chem & Mol Sci, Wuhan 430072, Peoples R China.;[Yang, Guangfu] Huazhong Normal Univ, Coll Chem, Wuhan 430072, Peoples R China.
通讯机构：
[Zhou, Xiang] W;Wuhan Univ, Coll Chem & Mol Sci, Wuhan 430072, Peoples R China.
关键词：
catechol;DNA damage;enzymes;oxidation;quinones
摘要：
A study was conducted to demonstrate the synthesis of a number of DNA crosslinking agents, such as bis(catechol) quaternary ammonium derives. It was found that these agents can crosslink DNA through an o-quinone intermediate, induced by oxidation. It was also found that these compounds are composed of two catechol monomers, acting as DNA cross-linking units and are joined by different linkers that act as DNA binding units. Positive charged linkers and quaternary ammonium derivatives were used in the study, to achieve high affinity to DNA. Aliphatic and aromatic chains were investigated, to determine their ability in performing favorable cross-linking reactions and to determine the relationship between agent flexibility and DNA cross-linking abilities.
语种：
英文
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Computational design and discovery of conformationally flexible inhibitors of acetohydroxyacid synthase to overcome drug resistance associated with the W586L mutation
作者：
Ji, Feng-Qin
* ;Niu, Cong-Wei;Chen, Chao-Nan;Chen, Qiong;Yang, Guang-Fu
（ ;...
期刊：
ChemMedChem ,2008年3(8):1203-1206 ISSN：1860-7179
通讯作者：
Ji, Feng-Qin
作者机构：
[Yang, Guang-Fu; Ji, Feng-Qin; Chen, Qiong; Chen, Chao-Nan] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Xi, Zhen; Niu, Cong-Wei] Nankai Univ, State Key Lab Elementoorgan Chem, Tianjin 300071, Peoples R China.;[Zhan, Chang-Guo] Univ Kentucky, Coll Pharm, Dept Pharmaceut Sci, Lexington, KY 40536 USA.
通讯机构：
[Ji, Feng-Qin] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
enzymes;inhibitors;molecular modeling;rational design
摘要：
(Figure Presented) Rational design: A series of 2-aroxyl-1,2,4-triazolo[1, 5-c]pyrimidine derivatives were computationally designed (see scheme) and synthesized as conformationally flexible AHAS inhibitors. These compounds could find use as new leads for combating drug resistance. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.
语种：
英文
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Blue Organic Light-emitting Supramolecular Microfibers: The Self-assembly of a 1,2,4-Triazolo[1,5-a]pyrimidine Derivative
作者：
Liu, Zu-Ming;Wang, Hong-Bo;Zhu, Xiao-Lei;Tu, Hai-Yang
* ;Yang, Guang-Fu
（ 期刊：
Molecules ,2008年13(4):855-863 ISSN：1420-3049
通讯作者：
Tu, Hai-Yang
作者机构：
[Yang, Guang-Fu; Liu, Zu-Ming; Zhu, Xiao-Lei; Wang, Hong-Bo; Tu, Hai-Yang] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Tu, Hai-Yang] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
1,2,4-triazolo[1,5-a] pyrimidine;acetohydrazone;synthesis;self-assembly;supramolecular
摘要：
The design and synthesis of 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine-2-thioaceto-(2-fluorobenzyl) hydrazone (TPTH), which self-assembled into supramolecularmicrofibers with blue organic light-emitting properties, is reported. This is the firstoccurrence of the molecular self-assembly of 1,2,4-triazolo[1,5-a]pyrimidine derivatives.
语种：
英文
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含1，2，4-***杂环的新型Strobilurins衍生物的合成及杀菌活性
期刊：
有机化学 ,2008年28(5):875-880 ISSN：0253-2786
通讯作者：
Zhao Pei-Liang
作者机构：
[杨光富; 章博; 王亚洲; 赵培亮] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Zhao Pei-Liang] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
会议名称：
中国化工学会农药专业委员会第十三届年会
会议时间：
2008-05-12
会议地点：
井冈山
会议论文集名称：
中国化工学会农药专业委员会第十三届年会论文集
关键词：
杀菌活性;晶体结构
摘要：
为了寻找新的高活性先导化合物，设计合成了14个未见文献报道的Strobilurins类衍生物，结构经MS，~1H NMR，元素分析确认．并用X—ray单晶衍射测定了（E）-3-甲氧基-2[（5-甲基-4-邻溴代苯亚甲基亚胺基-1，2，4-***）-3-硫亚甲基]-苯基丙烯酸甲酯（5i）的晶体结构，证实了分子中的两个C=C均为E-式构型．初步生物活性测试结果表明，在实验浓度下部分化合物具有一定的杀菌活性．
语种：
中文
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微波辅助下N-酰胺基-2-（4-氧代-4H-色烯-3-基）噻唑-4-酮类衍生物的平行合成及其杀虫活性
期刊：
有机化学 ,2008年28(8):1385-1392 ISSN：0253-2786
通讯作者：
Zhou Zhong-Zhen
作者机构：
[杨光富; 陈琼; 周中振] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[周中振] So Med Univ, Sch Pharmaceut Sci, Guangzhou 510515, Guangdong, Peoples R China.
通讯机构：
[Zhou Zhong-Zhen] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
微波辅助组合合成;噻唑-4-酮;色酮;杀虫活性
摘要：
利用微波辅助组合平行合成技术，色酮酰腙类衍生物与巯基乙酸发生缩合反应，成功地构建了N-酰胺基-2-（4-氧代-4竹色烯-3-基）噻唑-4-酮类化合物库．与常规加热方法相比较，反应时间由原来的8h缩短至9min，且收率大大提高．同时，在250μg／mL下，检测了其杀虫活性，初步生物测试结果表明部分化合物对红蜘蛛显示出良好的杀虫活性．
语种：
中文
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Syntheses and herbicidal activities of novel triazolinone derivatives
作者：
Luo, Yan-Ping;Jiang, Li-Li;Wang, Guo-Dong;Chen, Qiong;Yang, Guang-Fu
* （ 期刊：
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY ,2008年56(6):2118-2124 ISSN：0021-8561
通讯作者：
Yang, Guang-Fu
作者机构：
[Yang, Guang-Fu; Luo, Yan-Ping; Jiang, Li-Li; Wang, Guo-Dong; Chen, Qiong] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Yang, Guang-Fu] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
protoporphyrinogen oxidase;triazolinone;herbicide;crop selectivity
摘要：
Protoporphyrinogen oxidase (Protox, EC 1.3.3.4) has been identified as one of the most important action targets of herbicides. To search for novel Protox inhibitors, a series of title compounds 1, 2, and 3 were designed and synthesized by introducing three types of pharmacophores, cyclic imide, phenylurea, and (E)-methyl 2-methoxyimino-2-o-tolylacetate, into the scaffold of triazolinone. The bioassay results indicated that the resulting cyclic imide-type triazolinones 1 displayed much better herbicidal activities than phenylurea-type triazolinones 2. Most fortunately, compound 3, methyl 2-[3-methyl-(2-fluoro-4-chloro-5-ethylsulfonamidephenyl)-4,5-dihydro-5-oxo-1H-1, 2,4-triazol-4-yl]methyl-enephenyl-2-(E)-methoxyiminoacetate, was found to be the most promising candidate due to its comparable herbicidal activity at 75-150 g of active ingredient/ha with the commercial product sulfentrazone. On the basis of test results of herbicidal spectrum and crop selectivity, compound 3 could be developed as a postemergent herbicide used for the control of broadleaf weeds in rice fields. © 2008 American Chemical Society.
语种：
英文
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Synthesis, Fungicidal, and Insecticidal Activities of beta-Methoxyacrylate-Containing N-Acetyl Pyrazoline Derivatives
作者：
Zhao, Pei-Liang;Wang, Fu;Zhang, Ming-Zhi;Liu, Zu-Ming;Huang, Wei* ;...
期刊：
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY ,2008年56(22):10767-10773 ISSN：0021-8561
通讯作者：
Huang, Wei
作者机构：
[Yang, Guang-Fu; Wang, Fu; Liu, Zu-Ming; Huang, Wei; Zhang, Ming-Zhi; Zhao, Pei-Liang] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Huang, Wei] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
3,5-Diarylpyrazoline;beta-methoxyacrylate;fungicide;insecticide
摘要：
1-Acetyl-3,-5-diarylpyrazolines have received considerable interests from the fields of medicinal and agricultural chemistry due to their broad spectrum of biological activities. To discover new lead compounds exhibiting both fungicidal and insecticidal activities, a series of pyrazoline derivatives were designed and synthesized by introducing the β-methoxyacrylate pharmacophore into the scaffold of 1-acetyl-3,5-diarylpyrazoline. The fungicidal activities against Pseudoperoniospora cubensis, Sphaerotheca fuliginea, Botrytis cinerea, and Rhizoctonia solani and the insecticidal activities against Aphis medicagini, Nilaparvata legen, Mythima separata, and Tetranychus cinnabamus were screened. The most potent compound 13, 1-aceto-3-{m-[o-(E-1-methoxycarboxyl-2-methoxy)-1- yl]benzyloxy}phenyl-5-(benzo-[1,3]-dioxolyl)-4,5-dihydro- pyrazoline, was identified. Its fungicidal IC50 values against P. cubensis and S. fuliginea are 26.6 and 57.6 μg mL-1, respectively, while its insecticidal LC50 value against M. separata is 26.6 μg mL -1. These results indicated that compound 13 could be used as a lead for further developing new pyrazoline type products exhibiting both fungicidal and insecticidal activities. © 2008 American Chemical Society.
语种：
英文
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Syntheses of Diheterocyclic Compounds Based on 2-Thioacetohydrazide-5,7-dimethyl-1,2,4-triazolo[1,5-a]- pyrimidine
作者：
Liu, Zu-Ming;Chen, Qiong;Chen, Chao-Nan;Tu, Hai-Yang
* ;Yang, Guang-Fu
（ 期刊：
Molecules ,2008年13(6):1353-1360 ISSN：1420-3049
通讯作者：
Tu, Hai-Yang
作者机构：
[Yang, Guang-Fu; Liu, Zu-Ming; Chen, Qiong; Tu, Hai-Yang; Chen, Chao-Nan] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Tu, Hai-Yang] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
1,2,4-Triazolo[1,5-a]pyrimidine, triazole;1,3,4-oxadiazole;1,3,4-thiadiazoles
摘要：
The syntheses of some diheterocyclic compounds from 2-thioacetohydrazide- 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine (1) are described. Compound 1 can be converted into triazoles, 1,3,4-oxadiazoles, and 1,3,4-thiadiazoles. The structures of the intermediates and the target compounds were confirmed by 1H-NMR, MS and elemental analyses.
语种：
英文
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Discovery of a new insecticide lead by optimizing a target-diverse scaffold: Tetrazolinone derivatives
作者：
Luo, Yan-Ping
（ ;Yang, Guang-Fu
* 期刊：
Bioorganic & Medicinal Chemistry ,2007年15(4):1716-1724 ISSN：0968-0896
通讯作者：
Yang, Guang-Fu
（ 作者机构：
[Luo, Yan-Ping; Yang, Guang-Fu; Yang, GF] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Yang, Guang-Fu] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
1,3,4-Oxadiazole;1,3,4-Thiadiazole;Insecticidal activity;Lead compound;Tetrazolinone
摘要：
In order to discover lead compounds with novel action mechanism, a series of tetrazolinone derivatives bearing structurally diverse substituents, 1-aryl-4-substituted-1,4-di-hydro-5H-tetrazol-5-ones 2, 1-((5-(alkylthio)-1,3,4-oxadiazol-2-yl)methyl)-4-(substituted)- phenyl-1H-tetrazol-5(4H)-ones 5, and 1-((5-(alkylthio)-1,3,4-thiadiazol-2-yl)methyl)-4- (substituted)phenyl-1H-tetrazol-5(4H)-ones 7, were designed and synthesized in good yields by a multiple-step synthetic procedure. The results of greenhouse in vivo test indicated that all the target compounds did not displayed herbicidal activity, however, some of them exhibited excellent in vivo insecticidal activity against Tetranychus cinnabarinus at the concentration of 250 mg L-1. To our knowledge, this is the first report about the insecticidal activity of tetrazolinone derivatives, which indicated that the tetrazolinone scaffold could be identified as a novel insecticidal lead structure. The present work demonstrated that optimizing a target-diverse scaffold is an effective way to discover new lead compounds with new action mechanism or biological activity. © 2006 Elsevier Ltd. All rights reserved.
语种：
英文
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Preparation and characterization of inclusion complex of iprodione and beta-cyclodextrin to improve fungicidal activity
作者：
Zhu, Xiao-Lei;Wang, Hong-Bo;Chen, Qiong;Yang, Wen-Chao;Yang, Guang-Fu
* （ 期刊：
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY ,2007年55(9):3535-3539 ISSN：0021-8561
通讯作者：
Yang, Guang-Fu
作者机构：
[Yang, Guang-Fu; Zhu, Xiao-Lei; Chen, Qiong; Wang, Hong-Bo; Yang, Wen-Chao; Yang, GF] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Yang, Guang-Fu] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
Antifungal activity;Cyclodextrins;Inclusion complex;Iprodione;Molecular modeling
摘要：
The effect of β-cyclodextrin (β-CD) on the improvement of the fungicidal activity of iprodione has been investigated. The inclusion complexation of β-CD with iprodione has been prepared and characterized by integrating some analytical techniques (such as electrospray ionization-mass spectrometry, differential scanning calorimetry, thermogravimetry, x-ray diffraction, and scanning eletron microscopy) and molecular simulation methods. The β-CD/iprodione inclusion complex has exhibited different spectroscopic features and properties from iprodione. The stoichiometric ratio and stability constant describing the extent of formation of inclusion complexes have been determined by phase solubility studies. The calculated apparent stability constant of the iprodione/β-CD complex was 407.5 M-1. The obtained inclusion complexes were found to ignificantly improve the water solubility of iprodione, and there is a 4.7-fold increase in the presence of 13 mM β-CD as compared with the solubility of iprodione in deionized water in the absence of β-CD. The bioassay demonstrated that the complex displayed over two-fold increase of the fungicidal activity. In addition, the possible structure of the β-CD/iprodione complex was proposed according to the results of the molecular dynamic simulation. The present study provided useful information for a more rational application of iprodione, diminishing the use of organic solvents and increasing its efficacy. © 2007 American Chemical Society.
语种：
英文
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Rational design based on bioactive conformation analysis of pyrimidinylbenzoates as acetohydroxyacid synthase inhibitors by integrating molecular docking, CoMFA, CoMSIA, and DFT calculations
作者：
He, Yan-Zhen;Li, Yuan-Xiang;Zhu, Xiao-Lei;Xi, Zhen* ;Niu, Congwei;...
期刊：
Journal of Chemical Information and Modeling ,2007年47(6):2335-2344 ISSN：1549-9596
通讯作者：
Xi, Zhen
作者机构：
[Xi, Zhen] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;Nankai Univ, State Key Lab Elemento Organ Chem, Tianjin 300071, Peoples R China.
通讯机构：
[Xi, Zhen] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
摘要：
Pyrimidinylthiobenzoates constitute an important kind of herbicides targeting acetohydroxyacid synthase (AHAS, EC 2.2.1.6), which catalyze the first common step in branched-chain amino acid biosynthesis. Due to the symmetry of 4,6-dimethoxypyrimidyl, there are two kinds of conformation of pyrimidinylthiobenzoates: one's phenyl is left-extending (named conformation-L);the other's phenyl is right-extending (named conformation-R). On the basis of the assumption that 3D quantitative structure-activity relationship (QSAR) models derived from the bioactive conformation should give the best result, a strategy of density-functional-theory-based 3D-QSAR was proposed to identify the bioactive conformation of pyrimidinylthiobenzoates by integrating the techniques of molecular docking, comparative molecular field analysis (CoMFA), comparative molecular similarity indices analysis (CoMSIA), and density functional theory calculation. The combination of three criteria of q <sup>2</sup>, r<sup>2</sup>, and r<inf>pred</inf><sup>2</sup> obtained from CoMFA and CoMSIA analyses clearly indicated that conformation-R rather than conformation-L might be the bioactive conformation for pyrimidinylthiobenzoates. A further comparison between the two binding modes indicated that pyrimidinylthiobenzoates and sulfonylureas have very similar binding sites, such as Trp586, Arg380, and Pro192. However, Lys251 formed H bonds with sulfonylureas rather than pyrimidinylthiobenzoates. In addition, the orientation of phenyl groups of the two classes of compounds in the binding pocket were revealed to be opposite, which explained why the mutation of Pro192 displayed different sensitivity to sulfonylureas and pyrimidinylthiobenzoates. On the basis of the understanding of interactions between pyrimidinyl-thiobenzoates and AHAS, we designed and synthesized six 8-(4,6-dimethoxypyrimidin-2-yloxy)-4- methylphthalazin-1-one derivatives according to the 3D-QSAR models. The excellent correlation between the tested K<inf>i</inf> values against wild-type A. thaliana acetohydroxyacid synthase and the predicted IC<inf>50</inf> values demonstrated the high reliability of the established 3D-QSAR models. To our knowledge, this is the first report highlighting the binding mode of herbicidal pyrimidinylthiobenzoates, which consisted of the reported results of herbicide resistance. ©2007 American Chemical Society.
语种：
英文
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农药活性分子与作用靶标的相互作用研究
作者机构：
[杨光富] 农药与化学生物学教育部重点实验室华中师范大学化学学院
会议名称：
第五届全国化学生物学学术会议
会议时间：
2007-08
会议地点：
中国云南昆明
摘要：
<正>新农药创制研究是一项十分复杂的系统工程,农药活性分子药效的发挥虽然包括吸收、传导、代谢以及与作用靶标的相互作用等多个环节,但农药活性小分子与作用靶酶之间的选择性相互作用是影响其生物活性的最关键性因素。因此,研究农药活性分子与作用靶标的选择性相互作
语种：
中文
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杀菌剂Y5247的设计、合成及生物活性研究(摘要)
作者机构：
农药与化学生物学教育部重点实验室,华中师范大学化学学院,武汉,430079
会议名称：
第七届全国新农药创制学术交流会
会议时间：
2007-05-01
会议地点：
杭州
会议论文集名称：
第七届全国新农药创制学术交流会
关键词：
杀菌剂;药物设计;合成工艺;生物活性
摘要：
Strobilurin类杀菌剂是近年来开发成功的一类高效仿生杀菌剂,由于其广谱的杀菌活性,独特的作用机制和高效安全等优点,已成为当前杀菌剂开发中最重要的领域.一般而言,该类杀菌剂的分子结构可以分为三个部分:药效团部分、侧链结构部分和桥链结构部分.其中,修饰侧链结构是获得高活性化合物的一个重要途径.我们在保持药效团部分不变的基础上,对该类杀菌剂的侧链进行修饰,设计合成了结构多样性的杂环硫醚类衍生物.通过生物活性筛选发现,含苯并噻唑杂环的衍生物表现出很好的生物活性.以之为先导结构开展进一步的优化,设计、合成了一系列取代的苯并噻唑类Strobilurin衍生物.
语种：
中文
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大肠杆菌野生型和突变型AHASⅡ与新型取代嘧啶类抑制剂的相互作用
作者：
牛聪伟;陈超男;孙璐;陈琼;张楠;...
作者机构：
南开大学元素有机化学研究所,元素有机化学国家重点实验室,化学生物学系,天津,300071;华中师范大学农药与化学生物学教育部重点实验室,武汉,430079
会议名称：
第七届全国新农药创制学术交流会
会议时间：
2007-05-01
会议地点：
杭州
会议论文集名称：
第七届全国新农药创制学术交流会
关键词：
乙酰羟基酸合成酶;除草剂;抗性;嘧啶类抑制剂
摘要：
乙酰羟基酸合成酶(AHAS)催化支链氨基酸生物合成途径中的第一个关键酶.磺酰脲、咪唑啉酮、***嘧啶磺酰胺、嘧啶水杨酸等是以AHAS为作用靶标的四种最重要的商品化除草剂.由于长期的广泛使用,很多杂草对AHAS-抑制剂产生了抗性.为了更好地理解以及解决除草剂的抗性问题,我们考察了一类新型的化合物与野生及突变型AHAS的相互作用.研究发现,这类化合物对突变型AHAS Ⅱ和野生型酶有相似的抑制作用,表明这类化合物有望作为反抗性除草剂开发的先导.
语种：
中文
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Construction of a combinatorial library of 2-(4-oxo-4H-1-benzopyran-3-yl)-4-thiazolidinones by microwave-assisted one-pot parallel syntheses
作者：
Zhou, Zhong‐Zheng;Huang, Wei;Ji, Feng‐Qin;Ding, Ming‐Wu;Yang, Guang‐Fu
（ 期刊：
Heteroatom Chemistry ,2007年18(4):381-389 ISSN：1042-7163
通讯作者：
Yang, Guang-Fu
作者机构：
[Yang, Guang‐Fu; Huang, Wei; Zhou, Zhong‐Zheng; Ji, Feng‐Qin; Yang, GF; Ding, Ming‐Wu] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Yang, Guang-Fu] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
摘要：
A one‐pot liquid‐phase combinatorial synthesis of 2‐(4‐oxo‐4H‐1‐benzopyran‐3‐yl)‐4‐thiazolidinones bearing diverse substituents at the 3‐position under microwave irradiation was successfully performed using 3‐formyl chromone, primary amine, and mercaptoacetic acid as reactants. Compared to an identical library generated by conventional parallel synthesis, the microwave‐assisted parallel synthesis approach dramatically decreased the reaction time from an average of 9 h to 5 min, and substantially increased the product yields. The coupling of microwave technology with liquid‐phase combinatorial synthesis constitutes a novel and particularly attractive avenue for the rapid generation of structurally diverse libraries. © 2007 Wiley Periodicals, Inc. Heteroatom Chem 18:381–389, 2007; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20309
语种：
英文
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Design, synthesis, and fungicidal activities of new strobilurin derivatives
作者：
Huang, Wei;Zhao, Pei-Liang;Liu, Chang-Ling;Chen, Qiong;Liu, Zu-Ming;...
期刊：
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY ,2007年55(8):3004-3010 ISSN：0021-8561
通讯作者：
Yang, Guang-Fu
作者机构：
[Yang, Guang-Fu] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;Shenyang Res Inst Chem Ind, Agrochem Discovery Dept, Shenyang 110021, Peoples R China.
通讯机构：
[Yang, Guang-Fu] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
strobilurin;fungicide;benzothiazole;microwave irradiation
摘要：
Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin analogues with high activity against resistant pathogens, a series of new strobilurin derivatives bearing structurally diverse heterocycle side chains 3a−m and 4a−g were designed and synthesized via a microwave-assisted procedure. The advantages, such as good to excellent yields, shorter reaction times, mild reaction conditions, and simple purification procedures, distinguish the present synthetic protocol as a highly efficient method for the preparation of strobilurin thioether derivatives. Bioassays indicated that most of the compounds showed broad-spectrum fungicidal activity in vitro. Interestingly, as compared to the control of a commercial strobilurin fungicide, Kresoxim-methyl, compounds 3b, 3g, 4c, and 4d possessed remarkably higher in vitro fungicidal activity against six kinds of tested fungi. Exhilaratingly, compound 3g exhibited higher in vivo activity against Sphaerotheca fuliginea and Pseudoperoniospora cubensis than Kresoxim-methyl, and the in vivo fungicidal activities of compound 4d and Kresoxim-methyl against S. fuliginea and P. cubensis are at the same level. The present work demonstrated that strobilurin analogues containing benzothiazole side chains could be used as a lead structure for further developing novel fungicides.
Keywords: Strobilurin; fungicide; benzothiazole; microwave irradiation
语种：
英文
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Improved synthesis of 2-(3H)Benzothiazolethiones under microwave irradiation
作者：
Wei Huang;Ying Tan;Ming‐Wu Ding;Guang‐Fu Yang
（ 期刊：
Synthetic Communications ,2007年37(3):369-376 ISSN：0039-7911
通讯作者：
Yang, Guang-Fu
作者机构：
[Guang‐Fu Yang; Ying Tan; Wei Huang; Yang, GF; Ming‐Wu Ding] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol Minist Educ, Wuhan, Peoples R China.
通讯机构：
[Yang, Guang-Fu] C;Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol Minist Educ, Wuhan, Peoples R China.
关键词：
2-mercaptobenzothiazole;microwave irradiation;ortho-haloanline;potassium O-ethyl dithiocarbonate
摘要：
Abstract 2‐(3H)Benzothiazolethiones (2‐mercaptobenzothiazole) are prepared by an improved method, which utilizes microwave‐assisted cyclization of the corresponding ortho‐haloanlines with potassium O‐ethyl dithiocarbonate. By using microwave irradiation, the relative reactivity of 2‐chloroanilines was greatly improved to the same level as that of 2‐fluoroanilines and 2‐bromoanilines.
语种：
英文
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Development of an improved liquid phase, microextraction technique and its application in the analysis of flumetsulam and its two analogous herbicides in soil
作者：
Xu, Hui
* ;Pan, Wenhui;Song, Dandan;Yang, Guangfu
（ 期刊：
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY ,2007年55(23):9351-9356 ISSN：0021-8561
通讯作者：
Xu, Hui
作者机构：
[Yang, Guangfu; Song, Dandan; Xu, Hui; Pan, Wenhui] Cent China Normal Univ, Coll Chem, Ctr Anal & Testing, Minist Educ,Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构：
[Xu, Hui] C;Cent China Normal Univ, Coll Chem, Ctr Anal & Testing, Minist Educ,Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词：
liquid phase microextraction;high-performance liquid chromatography;flumetsulam and its two analogues;soil analysis
摘要：
An improved liquid phase microextraction (LPME) technique has been developed. As part of this technique, analytes were extracted into an extractant microdrop which was laid on the cone-shaped bottom of a PCR tube (polychloroprene rubber tube) but not at the needle tip of a microsyringe, and the sample vial and PCR tube were horizontally placed so that the extractant was not affected by the force of vertical orientation (gravity and floating force). The stability of the extractant microdrop increased greatly, and the selection of extractant was extended. In this work, flumetsulam and its two analogous herbicides were chosen as model analytes in investigating the feasibility of the new pretreatment method by coupling it to high-performance liquid chromatography (HPLC). Under the optimized experimental conditions, the linear range and the limits of detection (S/N= 3) were 0.01-5 μg/mL (r = 0.9997) and 0.8 ng/mL for flumetsulam, 0.002-5 μg/mL (r = 0.9994) and 0.5 ng/mL for analogue 1, and 0.002-1 μg/mL (r = 0.9993) and 0.5 ng/mL for analog 2, respectively. The inter-and intraday reproducibilities (RSD) were below 5.3 and 4.5%, respectively. Good recoveries that ranged from 79.4 to 115.0% were obtained in the analysis of real soil samples. The extraction efficiency of the improved method was 4-8 times higher than that of the conventional liquid phase microextraction method. The novel, simple, rapid, sensitive technique is very suitable for extraction of apolar and medium polar analyte in complex environmental samples. © 2007 American Chemical Society.
语种：
英文
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Erratum: Formation of supramolecular permethrin/ Β-cyclodextrin nanorods ( Journal of Chemical Physics (2006) 125 (111104))
作者：
Yang, Guang-Fu
* （ ;Wang, Hong-Bo;Yang, Wen-Chao;Gao, Daquan;Zhan, Chang-Guo
期刊：
JOURNAL OF CHEMICAL PHYSICS ,2007年126(5):059902 ISSN：0021-9606
通讯作者：
Yang, Guang-Fu
（ 作者机构：
[Yang, Guang-Fu] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan, Peoples R China.;Univ Kentucky, Coll Pharm, Dept Pharmaceut Sci, Lexington, KY 40536 USA.
通讯机构：
[Yang, Guang-Fu] C;Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan, Peoples R China.
关键词：
organic compounds;nanostructured materials
摘要：
This article was originally published online and print with incorrect footnotes for the first and fifth authors, Guang-Fu Yang and Chang-Guo Zhan. AIP apologizes for these errors. All online versions of the article have been corrected. Footnote b was removed, and the correct footnote for both authors appears below.
语种：
英文
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