Synthesis and antiproliferative evaluation of novel tetrahydrobenzo[4 ',5 ']thieno[3 ',2 ':5,6]pyrido[4,3-d] pyrimidine derivativest
作者:
Tang, Chu;Liang, Yongju;Bai, Shun;He, Hongwu;Chen, Yu;...
期刊:
RSC Advances ,2014年4(55):29187-29192 ISSN:2046-2069
通讯作者:
Yang, Guangzhong
作者机构:
[Tang, Chu; Yang, Guangzhong] South Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, Wuhan 430074, Peoples R China.;[Liang, Yongju; Fu, Liwu] Sun Yat Sen Univ, Ctr Canc, State Key Lab Oncol South China, Guangzhou 510060, Guangdong, Peoples R China.;[Bai, Shun; Chen, Yu] South Cent Univ Nationalities, Coll Chem & Mat Sci, Wuhan 430074, Peoples R China.;[He, Hongwu] Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.;[Yang, Guangzhong] South Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, 128 Minyuan Rd, Wuhan 430074, Peoples R China.
通讯机构:
[Yang, Guangzhong] S;South Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, 128 Minyuan Rd, Wuhan 430074, Peoples R China.
摘要:
A series of tetrahydrobenzo[4′,5′]thienophene[3′,2′:5,6]pyrido[4,3-d]pyrimidine-4-(3H)-one derivatives were synthesized and evaluated for their antiproliferative activities. Biological evaluation revealed that some compounds exhibited much stronger antiproliferative activity than the positive control Fluorouracil against KB and CEN2 cell lines. Compound 7a exhibited the highest antitumor activity against KB and CNE2 cell lines with IC50 values of 8.18 μM and 13.71 μM, respectively. The preliminary structure-activity relationships showed that introduction of tetrahydrobenzothieno as well as Schiff base units were favorable for the antiproliferative activity.
语种:
英文
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环三磷腈类阻燃剂的合成及应用研究进展
作者:
游歌云;程之泉;彭浩;贺红武
期刊:
应用化学 ,2014年31(9):993-1009 ISSN:1000-0518
作者机构:
[游歌云; 程之泉; 彭浩; 贺红武] 华中师范大学化学学院
关键词:
有机磷阻燃剂;六氯环三磷腈;阻燃机理;反应型;添加型
摘要:
简要介绍了制备环三磷腈类阻燃剂所需起始原料六氯环三磷腈的合成方法、合成及取代反应机理;介绍了环三磷腈阻燃剂的阻燃机理;着重阐述了近20年间反应型的羟基/氨基环三磷腈、环氧基环三磷腈、含不饱和双键的环三磷腈、羧基环三磷腈阻燃剂,以及添加型烷氧基环三磷腈、芳氧基环三磷腈的合成及阻燃应用,同时综述了其应用材料的热稳定性能和阻燃性能,并对其发展趋势作了总结和展望。
语种:
中文
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A WELL-DEFINED CYCLOTRIPHOSPHAZENE-BASED EPOXY MONOMER AND ITS APPLICATION AS A NOVEL EPOXY RESIN: SYNTHESIS, CURING BEHAVIORS, AND FLAME RETARDANCY
作者:
You, Geyun;Cai, Zhe;Peng, Hao;Tan, Xiaosong;He, Hongwu*
期刊:
Phosphorus, Sulfur, and Silicon and the Related Elements ,2014年189(4):541-550 ISSN:1042-6507
通讯作者:
He, Hongwu
作者机构:
[He, Hongwu; Peng, Hao; You, Geyun; Tan, Xiaosong; Cai, Zhe] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Hubei, Peoples R China.;[He, Hongwu] Cent China Normal Univ, Coll Chem, 152 Luoyu Rd, Wuhan 430079, Peoples R China.
通讯机构:
[He, Hongwu] C;Cent China Normal Univ, Coll Chem, 152 Luoyu Rd, Wuhan 430079, Peoples R China.
关键词:
Curing behavior;Cyclotriphosphazene;Epoxy resin;Flame retardancy;Organophosphorus
摘要:
A novel cyclotriphosphazene-based epoxy monomer, hexa-[4-(glycidyloxycarbonyl) phenoxy]cyclotriphosphazene (HGCP), was synthesized via a four-step synthetic route, and fully characterized by 1H, 13C, and 31P NMR spectroscopy, high-resolution mass spectrometry, and elemental analysis. Thermosetting systems based on HGCP with three curing agents, for example, 4,4′-diaminodiphenylsulfone (DDS), 4,4′-diaminodiphenylmethane (DDM), and dicyandiamide (DICY), were used for making a comparison of their thermal curing behaviors. The curing behaviors were measured by differential scanning calorimetry. Moreover, flame retardancy of HGCP thermosetting systems was estimated by Limiting Oxygen Index (LOI) and Vertical Burning Test (UL-94). The resulting HGCP thermosetting systems exhibited better flame retardancy than the common epoxy resins diglycidyl ether of bisphenol A (DGEBA) and the regular brominated bisphenol A epoxy resin (TBBA) cured by DDS, respectively. When HGCP was cured by DDS, its thermosetting system gave the most char residues, met the UL-94 V-0 classification, and had a limiting oxygen index value greater than 35.
语种:
英文
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A Convenient Synthesis and Biological Activity of Novel Pyrido[4,3-d] pyrimidin-4(3H)-ones
作者:
Ren, Qingyun;Shi, YanXia;Gu, Yucheng;Li, Baoju* ;He, Hongwu
期刊:
Journal of Heterocyclic Chemistry ,2014年51(2):285-290 ISSN:0022-152X
通讯作者:
Li, Baoju
作者机构:
[He, Hongwu; Gu, Yucheng; Ren, Qingyun] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Shi, YanXia; Li, Baoju] Chinese Acad Agr Sci, Inst Vegetables & Flowers, Beijing 100081, Peoples R China.;[Gu, Yucheng] Syngenta Jealotts Hill Int Res Ctr, Bracknell RG42 6EY, Berks, England.
通讯机构:
[Li, Baoju] C;Chinese Acad Agr Sci, Inst Vegetables & Flowers, Beijing 100081, Peoples R China.
摘要:
Fifteen novel 2-alkylamino-3-aryl-8-cyano-5-methyl-7-(methylthio)-pyrido[4, 3-d]pyrimidin-4(3H)-ones 6a, 6b, 6c, 6d, 6e, 6f, 6g, 6h, 6i, 6j, 6k, 6l, 6m, 6n, 6o were designed and have been successfully synthesized via tandem aza-Wittig and annulation reactions with the corresponding iminophosphorances 4, aryl isocyanate, and amines in good yields. Their structures were clearly verified by IR, 1H NMR, EI-MS spectroscopy and elemental analysis, and in the case of compound 6i, analyzed by single-crystal X-ray diffraction further. The preliminary results of an in vivo bioassay showed that some compounds display moderate antifungal activity. © 2013 HeteroCorporation.
语种:
英文
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A Highly Active CuI/TMEDA Catalytic System for the Coupling Reaction of Acid Chlorides with Terminal Alkynes under Solvent-Free Conditions
作者:
Yin, Weiyan* ;He, Haifeng;Zhang, Yani;Luo, Di;He, Hongwu
期刊:
Synthesis ,2014年46(19):2617-2621 ISSN:0039-7881
通讯作者:
Yin, Weiyan
作者机构:
[Zhang, Yani; Yin, Weiyan; Luo, Di] Hubei Acad Agr Sci, Natl Biopesticide Engn Res Ctr, Wuhan 430064, Peoples R China.;[He, Hongwu; He, Haifeng] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan, Hubei, Peoples R China.
通讯机构:
[Yin, Weiyan] H;Hubei Acad Agr Sci, Natl Biopesticide Engn Res Ctr, Wuhan 430064, Peoples R China.
关键词:
TMEDA;copper(I) iodide;ynones;acid chlorides;terminal alkynes
摘要:
A highly efficient copper(I) iodide/N,N,N',N'-tetramethylethylenediamine (CuI/TMEDA) catalytic system for the synthesis of ynones has been developed. A variety of terminal alkynes, including 4-iodophenylacetylene, were smoothly coupled with acid chlorides in the presence 2 mol% CuI and 5 mol% TMEDA to afford the corresponding ynones in good to excellent yields in a short time. It is noteworthy that the reaction is conducted under solvent-free conditions at room temperature.
语种:
英文
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A new spectrophotometric assay for measuring pyruvate dehydrogenase complex activity: A comparative evaluation
作者:
Ke, Chen-Juan;He, Ya-Hui;He, Hong-Wu;Yang, Xu;Li, Rui* ;...
期刊:
Analytical Methods ,2014年6(16):6381-6388 ISSN:1759-9660
通讯作者:
Li, Rui
作者机构:
[Yuan, Junlin; Li, Rui; Ke, Chen-Juan; Yang, Xu] Cent China Normal Univ, Sch Life Sci, Huibei Key Lab Genet Regulat & Integrat Biol, Wuhan 430079, Peoples R China.;[He, Ya-Hui] Pingdingshan Ctr Bur Qual & Tech Supervis Inspect, Ping Dingshan 467000, Peoples R China.;[He, Hong-Wu] Cent China Normal Univ, Sch Chem, Inst Pesticide Chem, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[Li, Rui] C;Cent China Normal Univ, Sch Life Sci, Huibei Key Lab Genet Regulat & Integrat Biol, Wuhan 430079, Peoples R China.
摘要:
Pyruvate dehydrogenase complex (PDHc) plays a key role in pyruvate decarboxylation, the transformation of pyruvate to acetyl-CoA. In this study, a new assay for measuring PDHc activity has been developed. 3-(4,5- Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) is adopted as the electron acceptor in this method, and the change in absorbance caused by the reduction of MTT by hydroxyethyl-TPP, which is the catalyzed product of pyruvate dehydrogenase (PDH, E1), within a certain period of time is measured to reflect PDHc activity. For further impartial evaluation of the characteristics of this newly developed assay, a series of comparative studies were also conducted with several commonly used assays of PDHc activity, including the conventional spectrophotometric assay of NADH accumulation, the p-iodonitrotetrazolium violet (INT)-coupled assay, the 2,6-dichlorophenolindophenol (2,6-DCPIP) assay, and the potassium ferricyanide assay. Results have proved that the spectrophotometric assay using MTT is highly sensitive and inexpensive with little interference from the sulfhydryl compound. In conclusion, the newly established assay is applicable for activity measurement not only in purified PDH and PDH in purified PDHc, but also in crude PDH solution prepared under certain conditions; hence, the assay can indirectly reflect the activity of PDHc activity. This journal is © the Partner Organisations 2014.
语种:
英文
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The design, synthesis and biological evaluation of novel thiamin diphosphate analog inhibitors against the pyruvate dehydrogenase multienzyme complex E1 from Escherichia coli
作者:
Feng, Lingling
( 冯玲玲 ) ;He, Junbo;He, Haifeng;Zhao, Lulu;Deng, Lingfu;...
期刊:
Organic & Biomolecular Chemistry ,2014年12(44):8911-8918 ISSN:1477-0520
通讯作者:
Wan, Jian
作者机构:
[Feng, Lingling; He, Hongwu; He, Junbo; Zhao, Lulu; He, Haifeng; Zhang, Li; Wan, Jian; Ren, Yanliang; Zhang, Lin] Cent China Normal Univ, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Coll Chem, Wuhan 430079, Peoples R China.;[He, Junbo] Wuhan Polytech Univ, Coll Food Sci & Engn, Wuhan 430023, Peoples R China.;[Deng, Lingfu] Cent China Normal Univ, Coll Life Sci, Wuhan 430079, Peoples R China.
通讯机构:
[Wan, Jian] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Coll Chem, Wuhan 430079, Peoples R China.
关键词:
design;synthesis and biological;novel thiamin diphosphate;Escherichia coli
摘要:
Pyruvate dehydrogenase multienzyme complex E1 (PDHc E1) is a potential target enzyme when looking for inhibitors to combat microbial disease. In this study, we designed and synthesized a series of novel thiamin diphosphate (ThDP) analogs with triazole ring and oxime ether moieties as potential inhibitors of PDHc E1. Their inhibitory activities against PDHc E1 were examined both in vitro and in vivo. Most of the tested compounds exhibited moderate inhibitory activities against PDHc E1 (IC<inf>50</inf> = 6.1-75.5 μM). The potent inhibitors 4g, 4h and 4j, had strong inhibitory activities with IC<inf>50</inf> values of 6.7, 6.9 and 6.1 μM against PDHc E1 in vitro and with inhibition rates of 35%, 50% and 33% at 100 μg mL<sup>-1</sup> against Gibberella zeae in vivo, respectively. The binding mode of 4j to PDHc E1 was analyzed by a molecular docking method. Furthermore, the possible interactions of the important residues of PDHc E1 with compound 4j were examined by site-directed mutagenesis, enzymatic assays and spectral fluorescence studies. The theoretical and experimental results are in good agreement and suggest that compound 4j could be used as a lead compound for further optimization, and may have potential as a new microbicide. This journal is ©the Partner Organisations 2014.
语种:
英文
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Design, synthesis and molecular docking of amide and urea derivatives as Escherichia coli PDHc-E1 inhibitors
作者:
He, Jun-Bo;Ren, Yan-Liang;Sun, Qiu-Shuang;You, Ge-Yun;Zhang, Li;...
期刊:
Bioorganic & Medicinal Chemistry ,2014年22(12):3180-3186 ISSN:0968-0896
通讯作者:
Wan, Jian
作者机构:
[Feng, Ling-Ling; Wan, Jian] Cent China Normal Univ, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Dept Chem, Wuhan 430079, Peoples R China.;Wuhan Polytech Univ, Coll Food Sci & Engn, Wuhan 430023, Peoples R China.
通讯机构:
[Wan, Jian] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Dept Chem, Wuhan 430079, Peoples R China.
关键词:
Amide and urea derivatives;Molecular docking;PDHc-E1 inhibitors
摘要:
By targeting the ThDP binding site of Escherichia coli PDHc-E1, two new 'open-chain' classes of E. coli PDHc-E1 inhibitors, amide and urea derivatives, were designed, synthesized, and evaluated. The amide derivatives of compound 6d, with 4-NO2 in the benzene ring, showed the most potent inhibition of E. coli PDHc-E1. The urea derivatives displayed more potent inhibitory activity than the corresponding amide derivatives with the same substituent. Molecular docking studies confirmed that the urea derivatives have more potency due to the two hydrogen bonds formed by two NH of urea with Glu522. The docking results also indicate it might help us to design more efficient PDHc-E1 inhibitors that could interact with Glu522. © 2014 Elsevier Ltd. All rights reserved.
语种:
英文
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2,5-取代-1,3,4-噁二唑衍生物的合成与杀菌活性
作者:
Liu Jianchao* ;Wang Weidong;He Hongwu
期刊:
有机化学 ,2014年34(7):1447-1451 ISSN:0253-2786
通讯作者:
Liu Jianchao
作者机构:
[Wang Weidong; Liu Jianchao; He Hongwu] Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[Liu Jianchao] C;Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
关键词:
4-噁二唑;吡啶环;噻唑环;杀菌活性
摘要:
利用生物活性亚结构拼接原理,将吡啶环、噻唑环引入到1,3,4-噁二唑母体结构中,设计并合成了一系列新型含吡啶(噻唑)的1,3,4-噁二唑衍生物。通过IR,1H NMR, EI-MS及元素分析等方法对所合成的化合物进行了结构表征。代表化合物2-(6-氯吡啶-3-甲硫基)-5-(吡啶-4-基)-1,3,4-噁二唑(I)经单晶 X 衍射证实了结构。初步测定了所合成化合物的杀菌活性,并比较了在1,3,4-噁二唑母体结构中引入噻唑杂环和引入吡啶杂环后其杀菌活性的差异。结果表明:目标化合物对测试的5种菌均具有一定的杀菌活性,对水稻纹枯病的抑制效果普遍优于对其它菌种的抑制效果;在1,3,4-噁二唑母体结构中引入噻唑杂环比引入吡啶杂环对其杀菌活性更有利。
语种:
中文
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Structural and Functional Analyses of a Sterol Carrier Protein in Spodoptera litura
作者:
Zhang, Lili;Li, Ding;Xu, Rui;Zheng, Sichun;He, Hongwu;...
期刊:
PLoS ONE ,2014年9(1):e81542- ISSN:1932-6203
通讯作者:
Wan, Jian
作者机构:
[Zhang, Lili; Xu, Rui; Zheng, Sichun] S China Normal Univ, Sch Life Sci, Guangdong Prov Key Lab Biotechnol Plant Dev, Guangzhou, Guangdong, Peoples R China.;[He, Hongwu; Feng, Qili; Wan, Jian; Li, Ding] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan, Peoples R China.
通讯机构:
[Wan, Jian] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan, Peoples R China.
关键词:
Cholesterol;Sterols;Fatty acids;Crystal structure;Larvae;Protein structure;Binding analysis;Molecular dynamics
摘要:
BACKGROUNDS: In insects, cholesterol is one of the membrane components in cells and a precursor of ecdysteroid biosynthesis. Because insects lack two key enzymes, squalene synthase and lanosterol synthase, in the cholesterol biosynthesis pathway, they cannot autonomously synthesize cholesterol de novo from simple compounds and therefore have to obtain sterols from their diet. Sterol carrier protein (SCP) is a cholesterol-binding protein responsible for cholesterol absorption and transport. RESULTS: In this study, a model of the three-dimensional structure of SlSCPx-2 in Spodoptera litura, a destructive polyphagous agricultural pest insect in tropical and subtropical areas, was constructed. Docking of sterol and fatty acid ligands to SlSCPx-2 and ANS fluorescent replacement assay showed that SlSCPx-2 was able to bind with relatively high affinities to cholesterol, stearic acid, linoleic acid, stigmasterol, oleic acid, palmitic acid and arachidonate, implying that SlSCPx may play an important role in absorption and transport of these cholesterol and fatty acids from host plants. Site-directed mutation assay of SlSCPx-2 suggests that amino acid residues F53, W66, F89, F110, I115, T128 and Q131 are critical for the ligand-binding activity of the SlSCPx-2 protein. Virtual ligand screening resulted in identification of several lead compounds which are potential inhibitors of SlSCPx-2. Bioassay for inhibitory effect of five selected compounds showed that AH-487/41731687, AG-664/14117324, AG-205/36813059 and AG-205/07775053 inhibited the growth of S. litura larvae. CONCLUSIONS: Compounds AH-487/41731687, AG-664/14117324, AG-205/36813059 and AG-205/07775053 selected based on structural modeling showed binding affinity to SlSCPx-2 protein and inhibitory effect on the growth of S. litura larvae.
语种:
英文
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The Synthesis and Characterization of a Novel Phosphorus-Nitrogen Containing Flame Retardant and its Application in Epoxy Resins
作者:
You, Geyun;Cheng, Zhiquan;Peng, Hao;He, Hongwu*
期刊:
Journal of Applied Polymer Science ,2014年131(22):n/a-n/a ISSN:0021-8995
通讯作者:
He, Hongwu
作者机构:
[He, Hongwu; Peng, Hao; You, Geyun; Cheng, Zhiquan] Cent China Normal Univ, Coll Chem, Inst Organ Synth, Wuhan 430079, Peoples R China.
通讯机构:
[He, Hongwu] C;Cent China Normal Univ, Coll Chem, Inst Organ Synth, Wuhan 430079, Peoples R China.
关键词:
applications;flame retardance;mechanical properties;synthesis and processing;thermogravimetric analysis
摘要:
ABSTRACT A novel, halogen‐free, phosphorus–nitrogen containing flame retardant 2[4‐(2,4,6‐Tris{4‐[(5,5‐dimethyl‐2‐oxo‐2λ5‐[1,3,2]dioxaphosphinan‐2‐yl)hydroxymethyl]phenoxy}‐(1,3,5)‐triazine (TNTP) was successfully synthesized in a three‐step process, and characterized by FTIR, NMR spectroscopy, mass spectra, and elemental analysis. A series of modified DGEBA epoxy resin with different loadings of TNTP were prepared and cured by 4,4‐diaminodiphenylsulfone (DDS). Thermal gravimetric analysis and vertical burning test (UL‐94) were used to evaluate the flame retardancy of TNTP on DGEBA epoxy resin. The results showed that TNTP had a great impact on flame retardancy. All modified thermosets by using TNTP exhibited higher Tg than pure DGEBA/DDS. The loading of TNTP at only 5.0 wt % could result in satisfied flame retardancy (UL‐94, V‐0) together with high char residue (27.3%) at 700°C. The addition of TNTP could dramatically enhance the flame retardancy of DGEBA epoxy resins, which was further confirmed by the analysis of the char residues by scanning electron microscopy and FTIR. Furthermore, no obviously negative effect was found on the Izod impact strength and flexural property of DGEBA epoxy resins when TNTP loading limited in 5.0 wt %. DGEBA/DDS containing 2.5 wt % TNTP could enhance Izod impact strength from 10.47 to 10.94 kJ m−2, and showed no appreciable effect on the flexural property (85.20 MPa) comparing with pure DGEBA/DDS (87.03 MPa). Results indicated that TNTP as a phosphorus–nitrogen synergistic intumescent flame retardant could be used for DGEBA epoxy resin. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014, 131, 41079.
语种:
英文
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新型四氢苯并[4,5]噻吩并[2,3-d]嘧啶酮衍生物的合成及其抗肿瘤活性
作者:
Chen Yu* ;Bai Shun;He Hongwu;Yang Guangzhong
期刊:
有机化学 ,2014年34(11):2362-2369 ISSN:0253-2786
通讯作者:
Chen Yu
作者机构:
[Chen Yu; Bai Shun] South Cent Univ Nationalities, Coll Chem & Mat Sci, Wuhan 430074, Peoples R China.;[He Hongwu] Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.;[Yang Guangzhong] South Cent Univ Nationalities, Coll Pharm, Wuhan 430074, Peoples R China.
通讯机构:
[Chen Yu] S;South Cent Univ Nationalities, Coll Chem & Mat Sci, Wuhan 430074, Peoples R China.
关键词:
噻吩并[2,3-d]嘧啶酮衍生物;抗肿瘤活性;Gewald 反应
摘要:
以环己酮为原料, 利用Gewald 反应合成了6个3-烷基-5,6,7,8-四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4-酮衍生物和17个3-亚苄基胺基四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4-酮衍生物, 通过~1H NMR、~(13)C NMR、IR 和MS 对所合成的化合物进行了结构表征, 并对所合成化合物进行了抗肿瘤活性的筛选. 结果表明4个化合物对人鼻咽癌细胞株(KB)和鼻咽鳞癌细胞株(CNE2)两种肿瘤细胞株表现出一定程度的抑制活性.
语种:
中文
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Synthesis and Herbicidal Activities of 2-Methylpropan-2-aminium O-Methyl l-(Substituted Phenoxyacetoxy)alkylphosphonates
作者:
Peng Hao;Deng Xiaoyan;Gao Ling;Tan Xiaosong;He Hongwu*
期刊:
高等学校化学研究:英文版 ,2014年30(1):82-86 ISSN:1005-9040
通讯作者:
He Hongwu
作者机构:
[Gao Ling; Deng Xiaoyan; Peng Hao; He Hongwu; Tan Xiaosong] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[He Hongwu] C;Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
关键词:
Herbicidal activity;Phosphonate;2-Methylpropan-2-aminium
摘要:
A series of 2-methylpropan-2-aminium O-methyl 1-(substituted phenoxyacetoxy)alkylphosphonates (5a-5o) was selectively synthesized by reacting the corresponding O,O-dimethyl 1-(substituted phenoxyacetoxy)-alkylphosphonates with an excess of 2-methylpropan-2-amine. The results of preliminary bioassays show that the title compounds exhibit moderate to good herbicidal activities against Brassica napus and Echinochloa crusgalli. Furthermore, compounds 5a-5j, which show much higher activities than compounds 5k-5o, were selected to further evaluate their post-emergence herbicidal activity at a dosage of 150 g/ha(1 ha=10000 m2). Especially, 2-methylpropan-2-aminium O-methyl 1-[2-(4-chloro-2-methylphenoxy)acetoxy]butylphosphonate(5h) shows 100% inhibitory effect on the growth of Brassica juncea and Amaranthus retroflexus, which is comparable with the commercial herbicide 2,4-dichlorophenoxy acetic acid(2,4-D). © 2014 Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH.
语种:
英文
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6-烷氨(氧)基-3-甲硫基-1H-吡唑并[3,4-d]嘧啶-4(5H)-酮衍生物的合成与生物活性
作者:
刘建超;梁英;贺红武
期刊:
应用化学 ,2014年31(8):922-927 ISSN:1000-0518
作者机构:
[刘建超; 贺红武] 华中师范大学化学学院;[梁英] 湖北省农业科学院
关键词:
aza-Wittig反应;吡唑并[3;4-d]嘧啶;杀菌活性;除草活性
摘要:
用六氯乙烷、三苯基膦和5-氨基吡唑衍生物一锅法合成关键中间体膦亚胺。再利用串联aza-Wittig 反应,加入对氯苯基异氰酸酯,进一步和烷基胺或取代酚反应合成了11个未见文献报道的6-烷氨(氧)基-3-甲硫基-1H-吡唑并[3,4-d]嘧啶-4(5H)-酮衍生物。通过1H NMR、EI-MS、IR和元素分析等方法对所合成的化合物进行了结构表征,并测试了它们的杀菌和除草活性。测试结果表明,部分化合物对稗草(barnyard grass)和油菜(Rape)均表现出了较好的抑制活性。
语种:
中文
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Lycopodium alkaloids from Lycopodium obscurum L.
作者:
Chen, Yu;He, Hong-Wu;Mei, Zhi-Nan;Yang, Guang-Zhong*
期刊:
Helvetica Chimica Acta ,2014年97(4):519-523 ISSN:0018-019X
通讯作者:
Yang, Guang-Zhong
作者机构:
[Chen, Yu] South Cent Univ Nationalities, Coll Chem & Mat Sci, Wuhan 430074, Peoples R China.;[He, Hong-Wu] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Mei, Zhi-Nan; Yang, Guang-Zhong] South Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, Wuhan 430074, Peoples R China.
通讯机构:
[Yang, Guang-Zhong] S;South Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, Wuhan 430074, Peoples R China.
关键词:
Lycopodium obscurum;Obscurumines F and G;Alkaloids
摘要:
Two new Lycopodium alkaloids, named obscurumines F and G (1 and 2, resp.), together with eleven known alkaloids, were isolated from the club moss Lycopodium obscurum L. Their structures were elucidated on the basis of spectroscopic analyses. Copyright © 2014 Verlag Helvetica Chimica Acta AG, Zürich.
语种:
英文
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Synthesis, Characterization and X-ray Crystal Structure of 2-Methylpropan-2-aminium Methyl ((4-Fluorobenzamido) (4-fluorophenyl)methyl)phosphonate·H_2O①
作者:
Gao Yu-Jiao;Deng Xiao-Yan;Peng Hao* ;He Hong-Wu
期刊:
Chinese Journal of Structural Chemistry ,2014年33(7):985-989 ISSN:0254-5861
通讯作者:
Peng Hao
作者机构:
[Peng Hao] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[Peng Hao] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
X-ray crystallography;benzamide;phosphonate
摘要:
A new crystal of 2-methylpropan-2-aminium methyl ((4-fluorobenzamido)(4-fluorophenyl)methyl)phosphonate has been prepared at room temperature and characterized by ~1H-NMR, ~(13)C NMR, IR, MS, elemental analysis and X-ray single-crystal determination. The compound crystallizes in monoclinic space group С2/с with a = 20.719(2), b = 11.8559(13), с = 18.176(2) A, β = 94.434(2)°, V= 4451.4(9) A~3, D_c = 1.317 Mg/m3, Z= 8, F(000) = 1864 and μ = 0.174 mm-1. The crystal packing is stabilized by intermolecular N-H ··· O and O-H···O hydrogen bonds, as well as by weak π-π stacking interactions.
语种:
英文
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Synthesis, Characterization and X-ray Crystal Structure of 4-Fluoro-N-(2-methyl-5-((2-(p-tolyloxy)acetamido)-methyl)pyrimidin-4-yl)benzamide
作者:
Deng Xiao-Yan;Peng Hao* ;He Hong-Wu
期刊:
Chinese Journal of Structural Chemistry ,2014年33(2):223-227 ISSN:0254-5861
通讯作者:
Peng Hao
作者机构:
[Peng Hao] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[Peng Hao] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
X-ray crystallography;acetamido;benzamide;pyrimidin
摘要:
A new crystal of 4-fluoro-N-(2-methyl-5-((2-(p-tolyloxy)acetamido)methyl)pyrimidin-4-yl)benzamide has been prepared at room temperature and characterized by ~1H NMR, ~(13)CNMR, IR, MS, elemental analysis and X-ray single-crystal determination. The compound crystallizes in monoclinic, space group P2_1/c with a = 17.226(5), b = 13.934(4), c = 17.262(5) A, b = 92.180(5)°, V = 4140(2) A~3, D_c = 1.311 g/cm~3, Z = 8, F(000) = 1712 and m = 0.095 mm~(-1). The molecular packing in the crystal is the result of N-H···O hydrogen bonds.
语种:
英文
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Design, synthesis and molecular modeling of novel N-acylhydrazone derivatives as pyruvate dehydrogenase complex E1 inhibitors
作者:
He, Jun-Bo;Feng, Ling-Ling
( 冯玲玲 ) ;Li, Jing;Tao, Rui-Juan;Ren, Yan-Liang;...
期刊:
Bioorganic & Medicinal Chemistry ,2014年22(1):89-94 ISSN:0968-0896
通讯作者:
Wan, Jian
作者机构:
[Feng, Ling-Ling; He, Jun-Bo; Ren, Yan-Liang; He, Hong-Wu; Wan, Jian; Li, Jing; Tao, Rui-Juan] Cent China Normal Univ, Dept Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[Wan, Jian] C;Cent China Normal Univ, Dept Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
关键词:
PDHc-E1 inhibitors;N-Acylhydrazone derivatives;Synthesis;Molecular modeling
摘要:
As potential inhibitors of pyruvate dehydrogenase complex E1 (PDHc-E1), a series of 19 1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-methyl-N′- (substituent)benzylidene-1H-1,2,3-triazole-4-carbohydrazide 4 has been synthesized and tested for their PDHc-E1 inhibitory activity in vitro. Some of these compounds such as 4a, 4g, 4l, 4o, 4p, and 4q were demonstrated to be effective inhibitors by the bioassay of Escherichia coli PDHc-E1. SAR analysis indicated that the PDHc-E1 inhibitory activity could be further enhanced by optimizing the substituted groups in the parent compound. Molecular modeling study with compound 4o as a model was performed to evaluate docking. The results of modeling study suggested a probable inhibition mechanism. © 2013 Published by Elsevier Ltd. All rights reserved.
语种:
英文
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Synthesis and Herbicidal Activities of Potassium Methyl 1-(Substituted Phenoxyacetoxy)alkylphosphonate
作者:
Wang Tao;Wang Wei;Peng Hao* ;He Hong-wu
期刊:
高等学校化学研究:英文版 ,2013年29(4):690-694 ISSN:1005-9040
通讯作者:
Peng Hao
作者机构:
[Wang Tao; Peng Hao; Wang Wei; He Hong-wu] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Peng Hao] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
Herbicidal activity;Phosphonate;Potassium salt
摘要:
A series of potassium methyl 1-(substituted phenoxyacetoxy)alkylphosphonates(9a-9o) was designed and synthesized. The results of preliminary bioassays indicate that most of the title compounds possess excellent pre-emergence and post-emergence herbicidal activities against Brassica napus, Amaranthus mangostanus, Medicago sativa, Echinochloa crusgalli, and Digitaria sanguinalis at a dosage of 1500 g/ha(1 ha=10000 m2). Especially, potassium methyl 1-(2,4-dichlorophenoxyacetoxy)-1-(4-methylphenyl)methylphosphonate(9g) and potassium methyl 1-(2,4-dichlorophenoxyacetoxy)-1-(furan-2-yl)methylphosphonate(9j) show the best herbicidal activity against five tested weeds with more than 85% inhibitory rate in pre-emergence. © 2013 Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH.
语种:
英文
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1,3,4-噁二唑衍生物的合成与活性研究
作者:
何海峰;贺红武;梁英;谭效松
作者机构:
华中师范大学化学学院 教育部农药与化学生物学重点实验室 武汉430079;湖北省农业科学院 湖北省生物农药工程研究中心 武汉430064
会议名称:
第十届全国新农药创制学术交流会
会议时间:
2013-05-01
会议地点:
济南
会议论文集名称:
第十届全国新农药创制学术交流会论文集
关键词:
杀菌剂;1,3,4-噁二唑衍生物;合成工艺;生物活性
摘要:
本文设计合成了一系列2-取代苯基-3-乙酰基-5-(2-氨基-4-甲基噻唑-5-基)-2,3-(2H)-1,3,4-噁二唑衍生物,所有化合物均通过了1H NMR、IR、MS及元素分析的表征.初步生测试结果表明它们具有一定的杀菌活性.
语种:
中文
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