黄烷酮衍生物的合成及杀菌活性

以取代苯甲醛为起始原料 ,经过肉桂酸衍生物合成了 7个黄烷酮衍生物 ,它们的结构分别经IR和1 H NMR确证。通过生物测试表明 ,部分化合物具有较好的杀菌活性     

Sterically Hindered Quaternary Phosphonium Salts (QPSs): Antimicrobial Activity and Hemolytic and Cytotoxic Properties

Structure–activity relationships are important for the design of biocides and sanitizers. During the spread of resistant strains of pathogenic microbes, insights into the correlation between structure and activity become especially significant. The most commonly used biocides are nitrogen-containing compounds; the phosphorus-containing ones have been studied to a lesser extent. In the present study, a broad range of sterically hindered quaternary phosphonium salts (QPSs) based on tri-tert-butylphosphine was tested for their activity against Gram-positive (Staphylococcus aureus, Bacillus cereus, Enterococcus faecalis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria and fungi (Candida albicans, Trichophyton mentagrophytes var. gypseum). The cation structure was confirmed to determine their biological activity. A number of QPSs not only exhibit high activity against both Gram-positive and -negative bacteria but also possess antifungal properties. Additionally, the hemolytic and cytotoxic properties of QPSs were determined using blood and a normal liver cell line, respectively. The results show that tri-tert-butyl(n-dodecyl)phosphonium and tri-tert-butyl(n-tridecyl)phosphonium bromides exhibit both low cytotoxicity against normal human cells and high antimicrobial activity against bacteria, including methicillin-resistant strains S. aureus (MRSA). The mechanism of QPS action on microbes is discussed. Due to their high selectivity for pathogens, sterically hindered QPSs could serve as effective tunable biocides.     

混合氨基酸铜络合物的杀菌活性

针对各种单一氨基酸铜络合物、混合氨基酸铜络合物及一些重金属混合氨基酸络合物，分别测定了它们对白粉病原菌、稻瘟病原菌和小麦根腐病原菌的毒性．实验结果表明，在混合氨基酸铜络合物中起主要杀菌作用的是谷氨酸铜、甘氨酸铜、丙氨酸铜和苏氨酸铜．     

Defensive sesquiterpenoids from a dipterocarp (Dipterocarpus kerrii)

Four sesquiterpenoids (2, 4, 7, and9) have been isolated and characterized from the termiticidal fraction ofDipterocarpus kerrii resin. The major constituent of this resin is -gurjunene (1).Presented at the Third Annual Meeting of the International Society of Chemical Ecology, June 21–24, 1986, University of California, Berkeley.     

N-联芳基酰胺类化合物的合成与杀菌活性研究

应用Suzuki偶联反应和缩合反应合成了8个结构新颖的N-联芳基酰胺类化合物,其结构经1HNMR、GC-MS进行了确证。初步杀菌活性研究结果表明所设计并合成的化合物具有一定的杀菌活性,如化合物9f和9g在500 mg/L剂量下,对小麦白粉病具有80%以上的防治效果;化合物9h在25 mg/L剂量下,对油菜菌核病菌的抑制活性达70%以上。     

3-(2,6-二氯苯基)-5-(1-吡咯烷酮基)-2,3-异唑啉的合成及抑菌活性研究

以2,6-二氯苯甲醛为原料,与盐酸羟胺反应生成2,6-二氯苯甲醛肟,经氯代得到氯代2,6-二氯苯甲醛肟,再和N-乙烯基吡咯烷酮进行1,3-偶极环加成反应,合成了3-(2,6-二氯苯基)-5-(1-吡咯烷酮基)-2,3-异唑啉。其结构经1 HNMR、13 CNMR及高分辨质谱表征。初步的离体生物活性测试结果表明,该异唑啉化合物对供试菌种普遍具有抑制作用,并且对水稻纹枯病菌的抑制率达到了95.8%。     

混合氨基酸铜络合物的杀菌活性

针对各种单一氨基酸铜络合物、混合氨基酸铜络合物及一些重金属混合氨基酸络合物，分别测定了它们对白粉病原菌、稻瘟病原菌和小麦根腐病原菌的毒性．实验结果表明，在混合氨基酸铜络合物中起主要杀菌作用的是谷氨酸铜、甘氨酸铜、丙氨酸铜和苏氨酸铜．     

链霉菌菌株4903抑菌除草活性的研究

从士样中分离筛选的链霉菌4903菌株的代谢产物同时具有抑菌、除草活性。链霉菌4903对荔枝炭疽病菌（Glomerella cingulata）和荔枝霜疫霉菌（Peronophythora litchii）的抑菌圈透明,抑菌圈直径达到和超过25mm。除草活性生测结果表明：在固体培养条件下,链霉菌4903菌株对小麦（Triticum aestivum）和油菜（Brassica campestris）有强烈的抑制作用,链霉菌4903菌株对小麦苗的抑制率为94%.对油菜根和苗的抑制率分别为97％和83％。     

9种药用植物内生或附生真菌的分离及其杀虫、抑菌活性

从9种药用植物的根、茎、叶、花中分离得到358株内生或附生真菌,其中9株真菌的发酵液对白纹伊蚊3龄幼虫的毒杀活性较强,24 h死亡率均达到80%以上;15株真菌的发酵液对至少1种供试病原真菌的菌丝生长抑制率超过50%;4株真菌的发酵液对5种供试细菌均有明显的抑菌活性.     

氟吗啉药效应用研究（Ⅰ）——室内生物活性测定

室内生测试验结果表明,氟吗啉对黄瓜霜霉病,葡萄霜霉病,番茄晚疫病,辣椒疫病,大豆疫霉根腐病具有较好的杀菌活性,５０ｍｇ／ｌ浓度下对黄瓜霜霉病菌孢子萌发抑制率为９３．５％,１００ｍｇ／ｌ浓度下对黄瓜霜霉病保护效果为１００％,治疗效果为９２．３％。