对苯二甲酰基硫脲衍生物的合成及其生物活性

合成了9个对苯二甲酰基硫脲化合物,采用1HNMR、IR、MS和元素分析对其结构进行了表征,并首次对其植物生长调节活性进行了测试.初步的生理活性研究表明,部分目标化合物,如N,N′-邻硝基苯基对苯二甲酰基硫脲等具有非常高的植物生长调节活性.     

2-(取代苯(苄)硫基)苯甲酸类化合物的合成及植物生长调节活性

[目的]二苯硫醚类化合物具有广泛的农药活性,但尚未有植物生长调节活性的报道,对二苯硫醚化合物的植物生长调节活性进行研究。[方法]以邻氯苯甲酸和取代苯硫酚(苄硫醇)为原料,一步合成目标化合物。[结果]合成了10个2-取代苯(苄)硫基苯甲酸衍生物。[结论]黄瓜子叶生根试验和室外苗木扦插繁殖试验表明二硫醚化合物具有优异的植物生长条件活性,活性优于吲哚丁酸。     

13种取代芳氧基丙酰氧基烃膦酸酯系列化合物生物活性初报

对13种(取代)芳氧基丙酰氧基烃基膦酸酯系列化合物进行了除草、杀虫、杀菌和植物生长调节活性的初步测定,结果表明:其双子叶植物抑制活性高(抑制率均>80％);抑制生根活性均达100％,且均产生愈伤组织;促进植株生长活性有2个化合物与IAA活性相近,1个化合物比IAA活性高34.9％;且杀虫和杀菌活性均很低(效果均<20％)     

4’-磺酰腙苯并-15-冠-5系列化合物的合成、表征及生物活性研究

苯并-15-冠-5经磺化反应、肼解反应和缩合反应,合成了3个4'-磺酰腙苯并-15-冠-5类化合物。产品经元素分析、红外光谱分析及~1HNMR分析,确定为目标化合物,并对这3个化合物进行了植物生长调节活性实验。结果表明,该类化合物有较好的植物生长调节活性。     

含吡啶环的双酰基硫脲衍生物的合成与生物活性

采用相转移催化法合成了6个含吡啶的双硫脲类新的化合物,其结构经1H NMR、IR、MS和元素分析表征。生物活性测试结果表明所设计化合物具有一定的植物生长调节活性。     

嘧啶胍的合成及生物活性

以嘧啶为起始原料,酸化后和单氰胺反应生成五种具有生物活性的嘧啶胍。通过红外光谱(IR)、核磁共振(1H NMR)、元素分析和熔点测定确定了各化合物的结构,研究了化合物对小麦赤霉病、烟草赤星病、西瓜枯萎病、马铃薯干腐病4种植物病原菌的生物活性,得到毒力回归方程及相关性系数、EC50和EC95值;还对小麦和萝卜生长调节的活性进行了研究。结果表明,该类化合物具有较好的抑菌活性和植物生长调节活性。     

α-硝基苯氧乙酰氧基烃基膦酸二甲酯的合成与生物活性

合成了五种不同α—硝基苯氧乙酰氧基烃基膦酸二甲酯的新化合物。用IR、~1H-NMR和元素分析等对目标化合物进行了表征。通过对其生物活性测试表明,某些化合物具有明显的植物生长调节活性。     

N′—（嘧啶—2—）苯甲酰硫脲的合成及其生物活性研究

合成了１０种含不同取代嘧啶环的苯甲酰硫脲类化合物，其中７个为未见文献报道的新化合物。其生物活性初步测定结果表明个４个目标化合物具有超高除草活性，１个具有良好的植物生长调节活性。     

咪唑啉酮类除草剂的创制经纬

咪唑啉酮类化合物是一类重要的除草剂 ,曾在世界特别是美国大豆市场上占有绝对的优势 ,但目前多为草甘膦取代。该类除草剂是由美国氰氨公司发现的 ,其创制经纬源于随机筛选 ,发现史如下 :　　化合物Ⅰ起初是作为抗痉挛用药合成的 ,氰氨公司于 1971年对其进行了除草活性的测定 ,发现其具有较好的除草活性 ,并进行进一步的研究。以化合物Ⅰ为先导化合物 ,在一系列先导展开中 ,发现了化合物ＡＣ94 377具有很好的植物生长调节活性 ;再经研究发现化合物Ⅱ同样具有促使植物生长的作用 ;更进一步的研究发现化合物Ⅲ的除草活性高于化合物Ⅰ。这也许…     

2-硬脂酰胺乙基乙基取代苯基磷酸酯的合成和生物活性

烷氧基磷酰二氯与取代苯酚、N-硬脂酰乙醇胺反应制备得到了6个新的标题化合物,其结构用核磁、元素分析进行了表征,并对它们的植物生长调节和杀菌活性进行了测定。     

Direct observation of freeze-thaw instability of latex coatings via high pressure freezing and cryogenic SEM

Despite its industrial importance, the subject of freeze-thaw (F/T) stability of latex coatings has not been studied extensively. There is also a lack of fundamental understanding about the process and the mechanisms through which a coating becomes destabilized. High pressure (2100 bar) freezing fixes the state of water-suspended particles of polymer binder and inorganic pigments without the growth of ice crystals during freezing that produce artifacts in direct imaging scanning electron microscopy (SEM) of fracture surfaces of frozen coatings. We show that by incorporating copolymerizable functional monomers, it is possible to achieve F/T stability in polymer latexes and in low-VOC paints, as judged by the microstructures revealed by the cryogenic SEM technique. Particle coalescence as well as pigment segregation in F/T unstable systems are visualized. In order to achieve F/T stability in paints, latex particles must not flocculate and should provide protection to inorganic pigment and extender particles. Because of the unique capabilities of the cryogenic SEM, we are able to separate the effects of freezing and thawing, and study the influence of the rate of freezing and thawing on F/T stability. Destabilization can be caused by either freezing or thawing. A slow freezing process is more detrimental to F/T stability than a fast freezing process; the latter actually preserves suspension stability during freezing. Presented at the 82nd Annual Meeting of the Federation of Societies for Coatings Technology, October 27–29, 2004 in Chicago, IL. Tied for first place in The John A. Gordon Best Paper Competition.     

Insect antifeedant properties of anthranoids from the genusVismia

Vismiones and ferruginins, representatives of a new class of lypophilic anthranoids from the genusVismia were found to inhibit feeding in larvae of species ofSpodoptera, Heliothis, and inLocusta migratoria.     

Many Drugs of Abuse May Be Acutely Transformed to Dopamine,Norepinephrine and Epinephrine In Vivo

It is well established that a wide range of drugs of abuse acutely boost the signaling of the sympathetic nervous system and the hypothalamic–pituitary–adrenal (HPA) axis, where norepinephrine and epinephrine are major output molecules. This stimulatory effect is accompanied by such symptoms as elevated heart rate and blood pressure, more rapid breathing, increased body temperature and sweating, and pupillary dilation, as well as the intoxicating or euphoric subjective properties of the drug. While many drugs of abuse are thought to achieve their intoxicating effects by modulating the monoaminergic neurotransmitter systems (i.e., serotonin, norepinephrine, dopamine) by binding to these receptors or otherwise affecting their synaptic signaling, this paper puts forth the hypothesis that many of these drugs are actually acutely converted to catecholamines (dopamine, norepinephrine, epinephrine) in vivo, in addition to transformation to their known metabolites. In this manner, a range of stimulants, opioids, and psychedelics (as well as alcohol) may partially achieve their intoxicating properties, as well as side effects, due to this putative transformation to catecholamines. If this hypothesis is correct, it would alter our understanding of the basic biosynthetic pathways for generating these important signaling molecules, while also modifying our view of the neural substrates underlying substance abuse and dependence, including psychological stress-induced relapse. Importantly, there is a direct way to test the overarching hypothesis: administer (either centrally or peripherally) stable isotope versions of these drugs to model organisms such as rodents (or even to humans) and then use liquid chromatography-mass spectrometry to determine if the labeled drug is converted to labeled catecholamines in brain, blood plasma, or urine samples.     

Ethanol and (−)-α-Pinene: Attractant Kairomones for Bark and Ambrosia Beetles in the Southeastern US

In 2002–2004, we examined the flight responses of 49 species of native and exotic bark and ambrosia beetles (Coleoptera: Scolytidae and Platypodidae) to traps baited with ethanol and/or (−)-α-pinene in the southeastern US. Eight field trials were conducted in mature pine stands in Alabama, Florida, Georgia, North Carolina, and South Carolina. Funnel traps baited with ethanol lures (release rate, about 0.6 g/day at 25–28°C) were attractive to ten species of ambrosia beetles (Ambrosiodmus tachygraphus, Anisandrus sayi, Dryoxylon onoharaensum, Monarthrum mali, Xyleborinus saxesenii, Xyleborus affinis, Xyleborus ferrugineus, Xylosandrus compactus, Xylosandrus crassiusculus, and Xylosandrus germanus) and two species of bark beetles (Cryptocarenus heveae and Hypothenemus sp.). Traps baited with (−)-α-pinene lures (release rate, 2–6 g/day at 25–28°C) were attractive to five bark beetle species (Dendroctonus terebrans, Hylastes porculus, Hylastes salebrosus, Hylastes tenuis, and Ips grandicollis) and one platypodid ambrosia beetle species (Myoplatypus flavicornis). Ethanol enhanced responses of some species (Xyleborus pubescens, H. porculus, H. salebrosus, H. tenuis, and Pityophthorus cariniceps) to traps baited with (−)-α-pinene in some locations. (−)-α-Pinene interrupted the response of some ambrosia beetle species to traps baited with ethanol, but only the response of D. onoharaensum was interrupted consistently at most locations. Of 23 species of ambrosia beetles captured in our field trials, nine were exotic and accounted for 70–97% of total catches of ambrosia beetles. Our results provide support for the continued use of separate traps baited with ethanol alone and ethanol with (−)-α-pinene to detect and monitor common bark and ambrosia beetles from the southeastern region of the US.     

Novel polyurethane coating technology through glycidyl carbamate chemistry

Glycidyl carbamate chemistry combines the excellent properties of polyurethanes with the crosslinking chemistry of epoxy resins. Glycidyl carbamate functional oligomers were synthesized by the reaction of polyfunctional isocyanate oligomers and glycidol. The oligomers were formulated into coatings with several amine functional crosslinkers at varying stoichiometric ratios and cured at different temperatures. Properties such as solvent resistance, hardness, and impact resistance were dependent on the composition and cure conditions. Most coatings had an excellent combination of properties. Studies were carried out to determine the kinetics of the curing reaction of the glycidyl carbamate functional oligomers with multifunctional and model amines. Detailed kinetic analysis of the curing reactions was also undertaken. The results indicated that the glycidyl carbamate functional group is more reactive than a glycidyl ether group. Presented at the 82nd Annual Meeting of the Federation of Societies for Coatings Technology, on October 27–29, 2004, in Chicago, IL.