芳氧苯氧丙酸酯类除草剂

芳氧苯氧丙酸类除草剂是在 2 ,4 -滴的基础上 ,通过进一步优化发现的。其发现史如下 :ＯＯＣＨＣＯ２ＣＨ３ＣＨ３ＮＣＦ３Ｃｌｈａｌｏｘｙｆｏｐ－ｍｅｔｈｙｌ（１９８１）２，４－Ｄ（１９４２） Ｄｏｗｃｏ２３３（１９７３）ＯＣＨ２ＣＯ２ＨＣｌＣｌＣｌＮ ＣｌＣｌＯＯＣＨ２ＣＯ２ＣＨ３ ｄｉｃｌｏｆｏｐ－ｍｅｔｈｙｌ（１９７４）ＣｌＣｌ ＯＣＨ２ＣＯ２ＨＣｌＣｌＯＯＯＣ２Ｈ５ＣＨ３ｑｕｉｚａｌｏｆｏｐ－ｅｔｈｙｌ（１９８３）ＯＮＮＣＨ３ＯＣ２Ｈ５ＯＯＯＮＯｆｅｎｏｘａｐｒｏｐ－ｅｔｈｙｌ（１９８２）ｆｌｕａｚ…     

芳氧苯氧羧酸类旋光性除草剂的研究进展

综述了芳氧苯氧羧酸酯类(APP)旋光性除草剂自20世纪70年代起至今的发展过程及其主要除草剂品种。总结了芳氧苯氧丙酸酯类除草剂及其重要中间体4-芳氧基苯酚、R-2-(4-羟基苯氧基)丙酸酯主要的合成方法,展望了芳氧苯氧羧酸酯类旋光性除草剂的发展前景。     

环己二酮类化合物的研究进展

环己二酮类除草剂以乙酰辅酶A羧化酶(ACCase)或对羟苯基丙酮酸双氧化酶(HPPD)为靶标酶,具有作用机理独特、安全、高效、低毒等特点,是目前最具发展潜力的除草性化合物之一。从靶标酶划分的角度综述了近几年来1,3-环己二酮类除草剂的研究近况,展望了其发展前景。     

芳氧苯氧丙酸酯类化合物的合成与生物活性研究

为寻找高效低毒的新农药,依据生物等排性原理,合成了10个芳氧苯氧丙酸酯类化合物,目标化合物的结构经1HNMR进行了确证。初步生测结果表明,这些化合物对禾本科杂草有很好的除草活性。     

二苯胺甲烷磺酸盐催化合成丙酸环己酯

以二苯胺甲烷磺酸盐为催化剂 ,对丙酸与环己醇之间的酯化反应进行了研究。实验结果表明反应的最佳条件为 :当丙酸用量为 0 .1mol时 ,醇酸比为 1 .4,二苯胺甲烷磺酸盐的用量为 0 .5g(约 2mmol) ,带水剂环己烷用量为 6mL ,反应 2 0min后酯收率达 88.4% ,催化剂重复使用五次仍保持较高活性。且所得产品无色透明 ,具有很高的纯度 ,经红外光谱进行了表征。     

含杂环甲胺基的氰基丙烯酸酯类光合作用抑制剂的合成和活性研究进展

氰基丙烯酸酯是一类PSII电子传递抑制剂,笔者发现在抑制剂分子疏水性基团苯环被吡啶替代能大大提高其抑制活性,对此先导结构进一步优化,设计合成以下系列新化合物:含2-氯(或烷氧基)-5-吡啶甲胺基的氰基丙烯酸酯、含2-氟-5-吡啶甲胺基的氰基丙烯酸酯、含2-氯-5-噻唑甲胺基的氰基丙烯酸酯、氮在吡啶环不同位置的吡啶甲胺基氰基丙烯酸酯、含烷硫基取代的吡啶甲胺基的氰基丙烯酸酯、含二茂铁甲胺基的氰基丙烯酸酯。生测结果表明:这些含杂环甲胺基的氰基丙烯酸酯类化合物对油菜等十字花科类杂草表现出很好的除草活性,且茎叶处理优于土壤处理。     

结构新颖的微生物源除草化合物及其作用特点

介绍了近期国内外引人注目的微生物源除草化合物。这些化合物具有新颖的化学结构、新奇的作用机理以及良好的除草活性。     

除草剂作用靶标的分类与使用

在除草剂使用日益普遍的今天,对其分类应重新评价,单纯按化合物分类、特别是使用时期分类已难以阐明使用中所发生的一系列问题。随着除草剂品种增多,使用者科技文化素质的提高,根据作用靶进行分类已显得更为重要,这种分类方法不仅有利于新化合物的筛选,而且有助于正确使用。     

Mechanisms of glycosyltransferases: the in and the out

Getting into a transition state: Glycosyltransferases retain a critical role in glycobiology. The design of potent glycosyltransferase inhibitors may be facilitated by considering the mechanistic evidence presented by Davies and Davis and co-workers that strengthens the case that retaining glycosyltransferases function through a single front-side, S(N)i-type mechanism.     

Intra-Articular Platelet-Rich Plasma Injections in Knee Osteoarthritis: A Review of Their Current Molecular Mechanisms of Action and Their Degree of Efficacy

Knee osteoarthritis (OA) is estimated to affect more than 10% of the population, with a lifetime risk of 45%. Contemporary guidelines advise control of body weight, therapeutic physical exercise, drug treatment (oral non-steroidal anti-inflammatory drugs, paracetamol, opioids), and mechanical aids (walking aids, braces, orthoses). Nevertheless, these treatments typically have only short-term benefits. Intra-articular corticosteroids are typically advised, but only for short-term pain alleviation, given that their benefits last only a few weeks. The efficacy of hyaluronic acid is controversial. When the aforesaid options fail, total knee arthroplasty is generally recommended as an efficacious treatment. However, it is costly and can involve medical and postoperative complications. Therefore, determining alternate safe and effective treatments for knee OA is paramount. Platelet-rich plasma (PRP) has lately been investigated for the treatment of knee OA. This article reviews recent knowledge concerning PRP’s molecular mechanisms of action. The effectiveness of intra-articular PRP injections in the knee joint remains controversial, although most recent publications show pain alleviation in the short term. Orthopedic surgeons treating people with knee OA are becoming increasingly interested in PRP, despite indecisive clinical data and basic science information. Further studies comparing PRP with placebo are required.     

Innovative Anti-CD38 and Anti-BCMA Targeted Therapies in Multiple Myeloma: Mechanisms of Action and Resistance

CD38 and B-cell maturation antigens (BCMAs) are prevalently expressed on neoplastic plasma cells in multiple myeloma (MM), making them ideal therapeutic targets. Anti-CD38 monoclonal antibodies, such as approved daratumumab and isatuximab, are currently the milestone in MM treatment because they induce plasma cell apoptosis and kill through several mechanisms, including antibody-dependent cellular cytotoxicity or phagocytosis. BCMA is considered an excellent target in MM, and three different therapeutic strategies are either already available in clinical practice or under investigation: antibody–drug conjugates, such as belantamab-mafodotin; bispecific T cell engagers; and chimeric antigen receptor-modified T cell therapies. Despite the impressive clinical efficacy of these new strategies in the treatment of newly diagnosed or multi-refractory MM patients, several mechanisms of resistance have already been described, including antigen downregulation, the impairment of antibody-dependent cell cytotoxicity and phagocytosis, T- and natural killer cell senescence, and exhaustion. In this review, we summarize the current knowledge on the mechanisms of action and resistance of anti-CD38 and anti-BCMA agents and their clinical efficacy and safety.     

无机纳米粒子增韧聚丙烯及其机理研究

综述了无机纳米粒子增韧聚丙烯的最新研究进展，阐述了不同纳米粒子对聚丙烯增韧效果的影响，介绍了无机纳米粒子的物理化学作用增韧机理和微裂纹化增韧机理。并对增韧改性聚丙烯的发展前景进行展望。     

The development of FtsZ inhibitors as potential antibacterial agents

The emergence and prevalence of bacterial resistance has resulted in a clear demand for novel antibacterial drugs. As a tubulin homologue, FtsZ is an essential cell-division protein in prokaryotic organisms and is showing increasing promise as a target for antibacterial drug discovery. This review describes the role of FtsZ in bacterial cytokinesis and various FtsZ inhibitors, with particular focus on their discovery, antibacterial activities, mechanisms of action, synthetic methods, and representative analogues.     

Coffee stain on textiles. Mechanisms of staining and stain removal

Coffee stains on textiles are mainly caused by the water-soluble and acidic colored substances in coffee. The acidic nature of coffee stain has been shown by ultraviolet and visible spectroscopy of coffee as a function of pH; ion-pair formation with a cationic surfactant and titration with Hyamine 1622 and a surfactant-specific electrode; and precipitation of the colored components in coffee with barium hydroxide as a barium salt. The permanence of coffee stains on textiles depends on the nature of the fibers. The affinity of coffee stain to fibers, indicated by resistance to detergency, increases in the order polyestern-nonanoyloxybenzenesulfonate, or Oxone® (DuPont, Wilmington, DE) obeys pseudo first-order kinetics. Oxone, a peroxysulfate triple salt, is a more powerful oxidant for coffee stain than sodium perborate, but its use is limited by the bleach fastness of dyes.     

HPPD抑制性除草剂的作用机制与品种Pyrasulfotole 的开发

综述了HPPD抑制除草剂的开发、生物化学靶标及最近商品化的、苗后防治麦类作物田阔叶杂草的新品种Pyrasulfotole。