由松香合成氨基噻二唑衍生物及其抑菌活性

以松香为起始原料,经歧化、提纯得脱氢枞酸、二氢枞酸;经Diels-Alder双烯加成得丙烯海松酸和马来海松酸。4种酸与硫代氨基脲关环得到4个新型氨基噻二唑衍生物化合物。通过红外、MS、1HNMR和元素分析对产物进行了表征。采用最低抑菌浓度法对目标产物的抑菌性能进行了测试,初步的结果显示,化合物都有一定的抑菌活性,特别是化合物5-脱氢枞基-2-氨基-1,3,4-噻二唑对金黄色葡萄球菌和表皮葡萄球菌具有良好的活性,对其最低抑菌质量浓度均为4 mg/L,而且比脱氢枞酸的活性高。     

松香基Schiff碱杂环衍生物的合成及抑菌活性

脱氢枞胺及降解脱氢枞胺分别与杂环甲醛在乙醇溶剂中缩合合成了6个松香基Schiff碱杂环衍生物(a_1/a_2、 b_1/b_2、 c_1/c_2),并对产物结构进行了IR、~1H NMR光谱表征确证。通过体外最低抑菌活性测试,结果表明,化合物c_1和c_2对金黄色葡萄球菌(Staphylococcus aureus)、表皮葡萄球菌(Staphylococcus epidermidis)、绿脓杆菌(Pseudomonas aeruginosa)和产气杆菌(Bacterium aerogenes)具有显著效果,其最低抑菌浓度(the Minimum Inhibitory Concentration)均为32μg·mL~(-1)。     

杂环金属配合物的合成及抑菌活性

为寻找新型广谱的抗菌素先导化合物,以5-溴呋喃-2-羧酸和2-四氢糠酸为起始原料合成了2种五元杂环铜配合物,利用¹H NMR、¹³C NMR对其结构及性质进行表征和分析,以平板菌落计数法测定铜配合物对大肠杆菌和金黄色葡萄球菌的抑制作用。初步体外抑菌活性显示,在0.038 mg/mL浓度下,目标化合物对两种细菌均具有较好的抑制活性。其中,5-(5-溴呋喃-2-基)-1,3,4-噻二唑铜(化合物4)的抑菌活性较强,其浓度与抑菌活性呈线性关系。     

诺蒎酮-噻唑腙类化合物的合成及抑菌活性

以β-蒎烯为原料经选择性氧化制得的诺蒎酮，再经羟醛缩合、酰腙化和环化反应得到15个的诺蒎酮-噻唑腙类化合物；采用1H NMR、13C NMR 和 HR-MS对所合成化合物的结构进行了表征；探索了所合成化合物对金黄色葡萄球菌、白色念珠菌和肺炎克雷伯氏菌的抑菌活性。结果表明，化合物2-{2-{6,6-二甲基-3-(4-硝基苯亚甲基)二环[3.1.1]庚-2-亚基}肼基}-4-(4-氟苯基)噻唑（Ⅲe）、4-{2-{2-{6,6-二甲基-3-(4-硝基苯亚甲基)二环[3.1.1]庚-2-亚基}肼基}噻唑-4-基}苯酚（Ⅲf）、2-{2-{3-(4-氟亚苄基)-6,6-二甲基双环[3.1.1]庚-2-亚基}肼基}-4-苯基噻唑（Ⅲg）和2-{2-{6,6-二甲基-3-(4-甲基亚苄基)二环[3.1.1]庚-2-亚基}肼基}-4-苯基噻唑（Ⅲj）对金黄色葡萄球菌抑菌效果显著，其最低抑菌质量浓度分别为3.51 μg/L、0.88 μg/L、7.03 μg/L和3.52 μg/L；化合物4-{2-{2-(3-亚苄基-6,6-二甲基二环[3.1.1]庚烷-2-亚基)肼基}噻唑-4-基}苯酚（Ⅲc）对白色念珠菌有较好的抑菌活性，最低抑菌质量浓度为28.12 μg/L；所有目标化合物对肺炎克雷伯氏菌的抑菌效果并不显著。从构效关系看：R1和R2上取代基的不同对化合物抑制金黄色葡萄球菌效果有明显的影响，当R1为强吸电子基团时能显著提高化合物的抑菌活性，其中化合物Ⅲf对金黄色葡萄球菌的抑制效果与硫酸卡纳霉素的抑制效果相当，具有潜在的开发价值。 关键词：-蒎烯；诺蒎酮；噻唑腙；抑菌活性     

1-(5-甲基-1,3,4-噻二唑基)-3-苯基硫脲的合成及抑菌实验研究

以四丁基溴化铵为催化剂、5-甲基-2-氨基-1,3,4-噻二唑和苯异硫氰酸酯为原料,在乙腈溶剂中合成了1-(5-甲基-1,3,4-噻二唑基)-3-苯基硫脲,确定了优化的工艺条件,并对产物的抑菌活性进行了初步研究.     

多基硫脲类Schiff碱的合成及生物活性与离子识别

以异硫氰酸苯酯、氨基硫脲、乙二胺、氨基脲和二乙撑三胺为原料,合成了异硫氰酸苯酯-氨基甲酰肼(PITCAM)、异硫氰酸苯酯-硫代氨基脲(PITCTSC),双异硫氰酸苯酯-1,2-二氨基乙烷(PITCE)和双异硫氰酸苯酯-二乙撑三胺(PITCD)4种多基硫脲类Schiff碱,其结构经1HNMR、IR、ESI-MS和元素分析进行表征.对4种合成的化合物进行抑制大肠杆菌、金黄色葡萄球菌以及欧文氏草生杆菌的生物活性测定,结果表明4种合成的多基硫脲类Schiff碱化合物均具有一定的生物抑菌活性,其中合成的化合物PITCAM的生物抑菌活性最好;测试其对不同金属离子的荧光响应光谱,实验结果表明PITCAM对Cu2响应明显.     

1, 2, 3-三唑类磺胺的合成及抗菌活性

以4-氨基苯磺酰胺为原料,其与氯乙酰氯反应得到中间体2-氯-N-(4-氨磺酰基苯基)乙酰胺(Ⅱ),然后Ⅱ与叠氮钠和端基炔"一锅法"反应合成了10个1, 2, 3-三唑类磺胺化合物(Ⅲa～j)。利用FTIR、1HNMR、13CNMR和ESI-MS对产物结构进行了表征。采用二倍稀释法测定了目标化合物的抗菌活性。结果表明:产物对金黄色葡萄球菌和大肠杆菌表现出一定的抗菌活性,特别是2-[4-(3-氟苯基)-1H-1,2,3-三唑-1-基]-N-(4-氨磺酰基苯基)乙酰胺(Ⅲh)对大肠杆菌的最低抑菌浓度MIC为0.25 mg/L,与阳性对照药环丙沙星相当。     

两种含二茂铁基schiff 碱的合成及其抑菌活性

通过乙酰基二茂铁与两种杂环胺(4-氨基安替比林,2-氨基-5-巯基-1,3,4-噻二唑)缩合合成了两种含二茂铁基的Schiff碱(a、b),产率分别为85.8%和72.6%,并通过IR、1HNMR及元素分析对其结构进行了确证。最后,将合成出的两种Schiff碱分别对3种细菌(金黄色葡萄球菌、大肠杆菌、枯草芽孢杆菌)进行了初步抑菌实验,将其结果与非杂环类Schiff碱Fc-C(CH3)NC6H5=(c)的抑菌性能做了比较。结果表明,Schiff碱对上述3种细菌都有抑制作用,且抑菌效果随着Schiff碱浓度的增大而增强。此外,杂环类Schiff碱(a、b)对上述3种细菌的抑菌活性明显优于非杂环类Schiff碱(c)。     

新型N-(1,3,4-噻二唑基)噻唑甲酰胺的合成及其杀菌活性

以5-烃基-2-氨基-1,3,4-噻二唑和2-甲基-4-三氟甲基噻唑-5-甲酰氯为原料,在三乙胺的作用下合成了新型结构的标题化合物,并且发现化合物中与1,3,4-噻二唑基相连的苯环上有吸电子取代基的产率比苯环上无取代基的产率低。产物的结构用IR、1HNMR、13CNMR和元素分析进行了表征。测试了目标化合物的杀菌活性,其对所测菌种均表现出一定的杀菌活性,而且1,3,4-噻二唑环上连有烷基的活性明显高于连有芳基的活性。     

松香树脂酸肟酯、噻二唑衍生物的合成与抑菌活性研究(摘要)

<正>松香是宝贵的可再生资源,树脂酸是松香的主要成分。松香树脂酸衍生物具有广泛的生物活性,在医药、农药等方面有着重要的用途。本文以松香、歧化松香和氢化松香为原料,经提纯、化学修饰,制备了含松香结构的肟酯、噻二唑衍生物等共15个化合物,其中10个新化合物;采用FTIR、1HNMR、元素分析、质谱以及单晶X射线四圆衍射等手段对这些化合物进行结构表征;同时以新洁尔灭和氨苄青霉素钠为参照物,采用最低抑菌浓度法(MIC)进行抑菌活性研究。     

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.     

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.     

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.     

Methyl 2,4,6-decatrienoates Attract Stink Bugs and Tachinid Parasitoids

Halyomorpha halys (Stål) (Pentatomidae), called the brown marmorated stink bug (BMSB), is a newly invasive species in the eastern USA that is rapidly spreading from the original point of establishment in Allentown, PA. In its native range, the BMSB is reportedly attracted to methyl (E,E,Z)-2,4,6-decatrienoate, the male-produced pheromone of another pentatomid common in eastern Asia, Plautia stali Scott. In North America, Thyanta spp. are the only pentatomids known to produce methyl 2,4,6-decatrienoate [the (E,Z,Z)-isomer] as part of their pheromones. Methyl 2,4,6-decatrienoates were field-tested in Maryland to monitor the spread of the BMSB and to explore the possibility that Thyanta spp. are an alternate host for parasitic tachinid flies that use stink bug pheromones as host-finding kairomones. Here we report the first captures of adult and nymph BMSBs in traps baited with methyl (E,E,Z)-2,4,6-decatrienoate in central Maryland and present data verifying that the tachinid, Euclytia flava (Townsend), exploits methyl (E,Z,Z)-2,4,6-decatrienoate as a kairomone. We also report the unexpected finding that various isomers of methyl 2,4,6-decatrienoate attract Acrosternum hilare (Say), although this bug apparently does not produce methyl decatrienoates. Other stink bugs and tachinids native to North America were also attracted to methyl 2,4,6-decatrienoates. These data indicate there are Heteroptera in North America in addition to Thyanta spp. that probably use methyl 2,4,6-decatrienoates as pheromones. The evidence that some pentatomids exploit the pheromones of other true bugs as kairomones to find food or to congregate as a passive defense against tachinid parasitism is discussed.     

2007～2008年世界塑料工业进展

收集了2007年7月～2008年6月世界塑料工业的相关资料,介绍了2007～2008年国外塑料工业的发展情况,提供了世界塑料产量、消费量及全球各类树脂的需求量及产能情况.按通用热塑性树脂(聚乙烯、聚丙烯、聚苯乙烯、聚氯乙烯、ABS树脂)、工程塑料(尼龙、聚碳酸酯、聚甲醛、热塑性聚酯、聚苯醚)、特种工程塑料(聚苯·硫醚、液晶聚合物、聚醚醚酮)、通用热固性树脂(酚醛、聚氨酯、不饱和聚酯树脂、环氧树脂)不同品种的顺序,对树脂的产量、消费量、供需状况及合成工艺、产品应用开发、树脂品种的延伸及应用的进一步扩展等技术作了详细介绍.     

2005～2006年国外塑料工业进展

收集了2005年7月～2006年6月国外塑料工业的相关资料,介绍了2005—2006年国外塑料工业的发展情况。提供了世界塑料产量、消费量及全球各类树脂生产量以及各国塑料制品的进出口情况。作为对比,介绍了中国塑料的生产情况。按通用热塑性树脂（聚乙烯、聚丙烯、聚苯乙烯、聚氯乙烯、ABS树脂）、工程塑料（聚酰胺、聚碳酸酯、聚甲醛、热塑性聚酯、聚苯醚）、通用热固性树脂（酚醛、聚氨酯、不饱和树脂、环氧树脂）、特种工程塑料（聚苯硫醚、液晶聚合物、聚醚醚酮）的品种顺序,对树脂的产量、消费量、供需状况及合成工艺、产品开发、树脂品种的延伸及应用的扩展作了详细的介绍。