三唑类除草剂的研究进展

三唑类化合物具有良好的生物活性,作为农用杀菌剂已使用多年,作为杀虫杀螨剂的例子也不少,但以前作为除草剂使用的实例较少,仅有杀草强和三唑磺,且未广泛使用。然而三唑类除草剂近几年得到了迅速的发展,尤其引人注目的是美国FMC公司开发的三唑啉酮类、陶氏益农公司开发的三唑并嘧啶磺酰胺类、日本吴羽化学公司开发的苯基三唑酰胺类以及日本中外制药公司开发的以CH 900为代表的三唑酰胺类化合物。这些化合物不仅具有新型的化学结构,而且在使用剂量方面亦具有优越性,可与超高效除草剂磺酰脲类相媲美。本文将对三唑类除草剂的研究进展按化学结构分类予以简要的介绍。     

杀菌剂开发的新进展

对近期开发的农用杀菌剂做了简要介绍.文中涉及三唑类、Strobilurin类、氨基酸衍生物、磺酰胺类及其他类化合物的结构、生物活性、作用机理以及部分化合物的创制经纬.     

N-(取代苯氧乙酰基)-3-氨基-二氢噻吩-2-酮衍生物的合成和生物活性

酰胺类化合物具有很高的药用活性,为了进一步研究酰胺衍生物的合成与性质,文中用3-氨基-二氢噻吩-2-酮盐酸盐与取代苯氧乙酸反应,得到N-(取代苯氧乙酰基)-3-氨基-二氢噻吩-2-酮衍生物。产物结构经IR、1H NMR和元素确证。对5种病原菌的抑菌活性进行了生物活性测试。合成中采用三氯氧磷为缩合试剂,采用一锅反应,简便易行,缩合试剂价廉易得、反应收率高,产物纯度较高,为此类新化合物的合成和筛选提供了依据。     

噻吩并[2,3-d]嘧啶衍生物的研究现状

2,4-二氨基噻吩并[2,3-d]嘧啶类衍生物和2-氨基-4-氧代噻吩并[2,3-d]嘧啶类衍生物是一些重要生物活性化合物的母体结构,对这两类化合物进行了归纳,并对其合成方法逐一进行了简要阐述.     

含炔键单元的寡聚噻吩类化合物的研究进展

寡聚噻吩类衍生物作为一个富电子体系通常表现出优越的电子传输性和光电性能,炔键作为一个直线型的富电子单元,引入到噻吩体系中可以增长体系的共轭度,增大体系中的刚硬核长度,同时还可以提高整个分子的平面规整度。含炔键单元的噻吩类化合物所具备的分子自组装性能和优异电子传输性已引起人们极大的关注。介绍了炔键在主链上,侧链上及含噻吩炔单元的环形、星形、X形与树枝形的寡聚噻吩类化合物的研究进展。阐述了它们的分子结构与液晶相态结构、光电性能、器件性能、自组装结构之间的关系。所有的研究表明该类化合物在有机分子器件方面有着重要的应用前景。     

噻吩类化合物电致发光材料的研究进展

较详细地对噻吩类化合物在电致发光材料领域的研究进展进行了综述。此类化合物包括聚合物类、齐聚物类、金属络合物类,其中对聚合物类的烷基取代噻吩和烷氧基取代噻吩进行了重点描述。并对噻吩类电致材料的发展前景作了评述。     

噻吩杀虫剂的研究进展

噻吩类化合物主要分为α-衍生物和β-衍生物,其应用领域广泛,其中噻吩类化合物在农药方面就有很广泛的应用,主要用于杀菌和杀虫,外国的很多研究显示噻吩类化合物对蚊蝇类卵、鳞翅目昆虫、幼虫具有显著的光活化毒杀效应,鳞翅目幼虫的生长发育起到抑制作用。概述了被文献报道的具有杀虫活性的部分噻吩类化合物,并对其发展前景进行展望。     

具有生物活性的异噻唑类化合物研究进展

异噻唑类化合物正逐渐成为农药的一个重要类别。按照化合物结构类型的不同将具有生物活性的异噻唑类化合物归纳为糖精类、胺类、异噻菌胺类似物、磺酰脲类、脲类、酰胺类及其他类共7类化合物。概述了这些类别中具有较好生物活性的化合物,同时介绍了研发此类化合物的创制经纬并对其研究趋势进行了展望,为以后该类化合物的研究提供了思路和依据。     

2-（2-噻吩）乙胺合成工艺研究

研究了2-（2-噻吩）乙胺的合成工艺.噻吩甲醛与丙二酸经Knoevenagel-Doebner缩合生成3-（2-噻吩）丙烯酸,收率87%.3-（2-噻吩）丙烯酸与氯化亚砜和氨作用生成3-（2-噻吩）丙烯酰胺,收率91%;铜盐催化下用水合肼还原3-（2-噻吩）丙烯酰胺生成3-（2-噻吩）丙酰胺,收率99%;3-（2-噻吩）丙酰胺经Hoffman降解得2-（2-噻吩）乙胺,收率64%.由核磁共振氢谱、质谱和液谱对产物及中间体的结构和纯度进行了表征.     

吡唑类衍生物杀菌活性研究进展

吡唑类化合物是一类具有良好杀菌活性的化合物.重点介绍了吡唑酰胺类、双杂环吡唑类、吡唑酰肼类、吡唑肟醚类、含金属配合物吡唑类、含硫吡唑类化合物的抗菌活性.研究表明:吡唑类化合物作为杀菌剂研究开发很有发展前景.     

具有农药活性的噻唑类化合物的研究进展

噻唑类化合物因具有良好的生物活性得到广泛的关注.重点介绍了近5年具有农药活性的噻唑酰胺、噻唑(硫)醚(砜)、噻唑丙烯腈、噻唑胺和哌啶噻唑类化合物进展,并对其生物活性及创制经纬进行了概述.     

海嘧啶对小白鼠S_(180)、EAC和H_(22)肿瘤细胞膜钠泵活性的影响

目的观察海嘧啶对小白鼠实体型肿瘤(S180)和腹水型肿瘤(EAC,H22)细胞膜钠泵活性的影响。方法荷瘤小鼠分为治疗组和对照组,分别测定各组瘤细胞膜钠泵活性。结果海嘧啶对小鼠S180、EAC及H22肿瘤细胞膜钠泵活性有明显的抑制作用。结论海嘧啶抗肿瘤的药理机制与其能够抑制肿瘤细胞膜钠泵活性有关。     

Factors affecting the acyltransfer activity of the lipase fromCandida parapsilosis in aqueous media

This study describes the influence of various factors on the hydrolysis and alcoholysis activities of the lipase fromCandida parapsilosis (Ashford), Langeron and Talice in aqueous media. Optimal activities were obtained at 45°C and pH 6–6.5. The influence of the nature of the substrate on the temperature activity profiles was observed. Total or partial recovery of the activities was obtained when methanol was added to the enzyme extract after thermal denaturation. A tyrosin residue appeared to be necessary for lipase function. Magnesium was a required metal cofactor. These activities were optimal in the presence of high amounts of water (water activity >0.9).     

1,3,4-噁二唑取代芳酰基硫脲的合成及杀菌活性研究

设计合成了10个1,3,4-噁二唑取代的芳酰基硫脲类化合物,所有化合物的结构经IR,^1HNMR及元素分析确证。初步生物测试结果表明,大多数化合物具有较好的杀菌活性。     

丹皮酚合成过程中抑菌活性的变化研究

研究了在丹皮酚的合成过程中,原料间苯二酚、中间产物2,4-二羟基苯乙酮及主产物丹皮酚对11种植物病原真菌的抑菌活性,并通过抑菌活性的变化来推测影响抑菌活性的主要官能团.结果表明:0.5g·L-1的2,4-二羟基苯乙酮对11种真菌的抑菌率大于或等于同浓度丹皮酚的抑菌率,两者均远远大于同浓度间苯二酚的抑菌率.由此可推测,酚类分子中乙酰基的引入对抑菌活性起到了非常重要的作用,而酚羟基的甲基化的作用却并不显著.该结论对寻求具有更高抑菌活性的酚类衍生物有着非常重要的意义.     

姜黄素衍生物的生物活性研究概况

姜黄素衍生物具有杀虫、抑菌、抗病毒、消炎抗氧化、抗癌等多种生物活性。概述了对姜黄素芳环及芳环上酚羟基、β-二酮、活泼亚甲基进行修饰,或者对去掉活泼亚甲基和一个羰基后的1,4-戊二烯-3-酮类化合物进一步修饰后,得到的化合物具有较高的生物活性,并展望了其未来的发展前景。     

Hepatic Δ9 and Δ6 desaturase activities during the recovery period following carbon tetrachloride poisoningdesaturase activities during the recovery period following carbon tetrachloride poisoning

The liver microsomal Δ⁹ and Δ⁶ desaturase activities have been studied in rats with carbon tetrachloride-induced hepatitis. Immediately after poisoning, significant decreases were observed for both types of desaturase activity. However, recovery kinetics were slower for the Δ⁶ desaturase than for the Δ⁹ desaturase. The activities of NADH-ferricyanide and NADH-cytochrome C reductases, proteins involved in the electron transfers associated with microsomal desaturation, were also measured. There was a fall in both activities after poisoning, but this decrease was less than that of the desaturase activities.     

二胍基钛配合物对苯乙烯聚合反应的催化性能研究

初步研究了所合成的五个二胍基钛配合物与改性的甲基铝氧烷(MMAO)组成的摧化体系对苯乙烯聚合的催化性能。结果表明:二胍基钛二氯化物和MMAO组成的催化体系可以催化苯乙烯的立体规整聚合,得到高间同含量的聚苯乙烯。     

酰腙类化合物生物活性研究进展

酰腙类化合物由于其广泛的生物活性,在农药与医药研究领域占有重要的地位。主要用作杀虫剂、杀菌剂、除草剂、消炎剂、镇痛剂。多年来酰腙类化合物的合成和生物活性研究一直是精细化工领域研究开发的重要方向之一。本文综述了近年来该类化合物生物活性方面的研究近况。     

Diesel fuel as a solvent for the lipase-catalyzed alcoholysis of triglycerides and phosphatidylcholine

The abilities of three commercially available lipases—Lipozyme IM 20, Amano PS-30, and Amano CE—to synthesize fatty acid ethyl esters via the alcoholysis of soy triglycerides (TG) and phosphatidylcholine (PC) in grade No. 2 diesel fuel were investigated. All three enzyme preparations were active in water-saturated diesel fuel, synthesizing fatty acid esters from both TG and PC. Response surface methodology, based on a Modified Central Composite design, was employed to examine the coordinate effects of lipid, water, and ethanol concentrations on enzyme activities and to identify conditions yielding maximum alcoholysis. For all three enzymes, optimal activities toward TG occurred at added water concentrations of less than 0.3 M. With PC as substrate, optimal enzyme activities occurred at added water concentrations as much as tenfold greater than this, and the amount of water required for maximum activity was proportional to the substrate concentration. For both substrates the enzyme activities were generally reduced as ethanol concentrations rose. The exceptions to this were the Lipozyme-TG combination, where activity increased with increasing ethanol concentrations, and the PS-30-PC combination, where activity was roughly constant across the range of water and ethanol concentrations examined. Hydrolytic activities of the enzymes in aqueous reactions were poor predictors of transesterification activity in organic solvent: the aqueous hydrolytic activities of CE and PS-30 toward TG were roughly comparable, and 25 to 50 times greater than that of IM 20. However, in the alcoholysis of TG in diesel fuel the order of activities was PS-30>IM 20>CE. The activities of Lipozyme and CE toward PC were similar to one another, and PS-30 was considerably less active on this substrate. CE lipase was more active toward PC than toward TG. Lipozyme displayed comparable activity toward the two substrates. PS-30 was considerably more active on TG than on PC. Degrees of conversion were consistent with the transesterification of only one fatty acid of TG, and slightly greater than one fatty acid for PC. Preliminary studies indicated that for CE and PS-30, but not for Lipozyme IM 20, the degree of conversion of TG, but not PC, could be significantly increased by the further provision of ethanol. Expansion of this work could lead to a method for the production of simple fatty acid esters, which are suitable as diesel fuels, from multicomponent agricultural materials containing TG and PC.