期刊：
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS,2015年190(7):972-977 ISSN：1042-6507
通讯作者：
Peng, Hao
作者机构：
[He, Hongwu; Peng, Hao; Gao, Yujiao; Wang, Tao] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan, Hubei, Peoples R China.;[Wang, Tao] Jiangxi Normal Univ, Coll Chem & Chem Engn, Nanchang, Jiangxi, Peoples R China.
通讯机构：
[Peng, Hao] C;Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan, Hubei, Peoples R China.
关键词：
Synthesis;herbicidal activity;phosphinate
摘要：
A series of sodium methyl(α-(substituted phenoxyacetoxy)alkyl)phosphinates was designed and synthesized. Their structures were confirmed by IR, 1H NMR and elemental analysis, and some of them were further confirmed by MS. The results of bioassay showed that most of title compounds exhibited moderate to good herbicidal activities against the root of barnyard grass and rape at 10∼100 mg/L.
摘要：
以商品化的杀菌剂噻唑菌胺和噻氟酰胺为先导,保持噻唑环活性结构,在噻唑环的4位引入酯基,设计合成了9个新型的4-取代苯甲酰氧基-2-取代苯甲酰氨基噻唑衍生物,中间体2-亚氨基-4-噻唑烷酮由简便易得的原料溴乙酸乙酯与硫脲一步合成.用IR、1 H NMR、13 C NMR、MS和元素分析等对合成的噻唑酰胺化合物结构进行了表征.并对其杀菌和抗肿瘤生物活性进行了测试,初步的研究结果表明,该类化合物基本上没有抗肿瘤活性,但部分化合物对小麦赤霉病和黄瓜灰霉病有较好的抑制效果.
摘要：
To identify new antifungal lead compound based on inhibitors of pyruvate dehydrogenase complex E1, a series of 5-iodo-1,4-disubstituted-1,2,3-triazole derivatives 3 were prepared and evaluated for their Escherichia coli PDHc-E1 inhibitory activity and antifungal activity. The in vitro bioassay for the PDHc-E1 inhibition indicated all the compounds exhibited significant inhibition against E. coli PDHc-E1 (IC50 < 21 mu M), special compound 3g showed the most potent inhibitory activity (IC50 = 4.21 +/- 0.11 mu M) and was demonstrated to act as a competitive inhibitor of PDHc-E1. Meanwhile, inhibitor 3g exhibited very good enzyme-selective inhibition of PDHc-E1 between pig heart and E. coli. The assay of antifungal activity showed compounds 3e, 3g, and 3n exhibited fair to good activity against Rhizoctonia solani and Botrytis cinerea even at 12.5 mu g/mL. Especially compound 3n (EC50 = 5.4 mu g/mL; EC90 = 21.1 mu g/mL) exhibited almost 5.50 times inhibitory potency against B. cinerea than that of pyrimethanil (EC50 = 29.6 mu g/mL; EC90 = 113.4 mu g/mL). Therefore, in this study, compound 3n was found to be a novel lead compound for further optimization to find more potent antifungal compounds as microbial PDHc-E1 inhibitors. (C) 2015 Elsevier Ltd. All rights reserved.
关键词：
Herbicide;Ultrastructure;Gene transcript;N and P absorption
摘要：
Both 2-[(2,4-dichlorophenoxy)acetoxy](methy)lmethyl-5,5-dimethyl-1,3,2-dioxaphosphinan-2-one (termed as IIa) and 2-[(4-chloro-2-methyl-phenoxy)-acetoxy](methyl)methyl-5,5-dimethyl-1,3,2-dioxaphosphinan-2-one (termed as IIr) are novel herbicide candidates that positively affect herbicidal activity via the introduction of a phosphorus-containing heterocyclic ring. This report investigated the mechanism of IIa and IIr on weed control in the model plant Arabidopsis thaliana at physiological, ultrastructural and molecular levels. IIa and IIr significantly inhibited the growth of A. thaliana and altered its root structure by inhibiting energy metabolism and lipid or protein biosynthesis. These compounds also significantly affected the absorption of nitrogen and phosphorus by down-regulating the transcripts of nitrate transporterrelated genes, ammonium transporter-related genes and phosphorus transporter-related genes. (C) 2015 Elsevier Inc. All rights reserved.
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.
摘要：
Convenient approach to synthesize tertiary α-hydroxy cyclic phosphonates catalyzed by potassium carbonate under solvent-free conditionsAll authorsChubei Wanga*, Jianwei Zhoua, Jianfeng Liub, Liangliang Chua & Hongwu HecDOI:http://dx.doi.org/10.1080/10426507.2013.860532Published online:15 September 2014PowerPoint slideOriginal jpg (14.00KB)Display full sizeA new environmentally benign, convenient, and easy method for the synthesis of tertiary α-hydroxy cyclic phosphonates was developed. In the presence of potassium carbonate, aromatic/heteroaromatic ketones and base-sensitive ketones can react with phosphite to form tertiary α-hydroxyphosphonates under solvent-free and mild conditions.
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.
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.
