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首页 > 新闻咨询 > Revysol –创新型杀菌剂

Revysol –创新型杀菌剂

Release Time:2020-03-24
巴斯夫开发了首个异丙醇-吡唑可用于保护农作物免受真菌病害的Revysol,从而打破了三唑类杀菌剂的生产模式。

 
当病原体的孢子感染植物时,会形成细分支细丝的菌丝体,其外层由柔性膜组成。仔细观察该膜的分子结构,可以发现它处于恒定的流体运动中,受大量嵌入的麦角固醇分子的调节。麦角固醇是在真菌细胞内部产生的,其中的酶D-14脱甲基酶起着至关重要的作用。这是去甲基化抑制剂(DMI)杀真菌剂的目标。
 
自1980年代以来,已经有许多DMI杀菌剂可用,几乎全部属于三唑类化合物。尽管抗药性的出现(在产生D-14脱甲基酶的靶位点发生突变)正在挑战其有效性,但它们构成了作物保护策略的骨干。由于具有这种作用方式的新分子超过十年没有投放市场这一事实使情况更加复杂。
 
巴斯夫从合成数千种新的三唑分子开始着手解决这一问题。该公司的科学家发现了一个分子,其中的三唑头位于稀异丙醇单元的颈部。该结构使分子易于呈现不同的构象-未结合(直链)和结合(钩接)。

如右图所示,在Revysol分子中,三唑的头部(蓝色)位于一个薄的异丙醇单元(黄色)的颈部,当“头部”向上或向下弯曲时,该分子呈现不同的构象。 '颈部'。

当Revysol分子接近D-14脱甲基酶的位点时,它切换为结合(钩接)的形式,即使形成了靶位点突变,它也具有强大的结合特性。它停止了麦角固醇的产生,在真菌膜上出现裂缝,病原体死亡。
 
施用后,Revysol会被叶子迅速吸收,使其耐雨。由于叶片内部形成了水库,Revsol从中逐渐释放到植物的水传输系统中,杀菌剂渗透到植物中以提供广泛而持久的保护。据巴斯夫称,这代表了“疾病控制的新水平”。该公司认为,该产品将成为许多重要作物(包括谷物,大豆和玉米以及水果和蔬菜)中抗药性管理的重要工具。它还有望为草皮管理和种子处理市场提供新的选择。
 
由于采用了新的筛选系统,Revysol的设计还可以满足较高的法规要求。巴斯夫已在60个国家/地区申请了Revysol的40多种作物的注册。 Revysol的监管档案已于2016年3月提交给欧盟,并于2017年8月在美国,加拿大和墨西哥获得了监管批准。2019年3月宣布了欧盟的批准,现在预计今年将在2019 / 2020年生长季节。 Revysol将以定制配方提供给全球农民。

Hailed as BASF’s next blockbuster, Revysol has the potential of reaching peak sales above €1 billion. Interestingly, the company’s manufacturing plant in Hannibal, Missouri (USA) has been selected as Revysol’s production site (pictured). This choice emphasizes the strategic importance of the new fungicide to North American markets. With an investment in the double-digit million Euro range, BASF has enhanced an existing manufacturing system to produce the new active ingredient.
 
“We are proud that Hannibal is the first site to produce Revysol,” said Anne Berg, Vice President Manufacturing Americas, BASF’s Agricultural Solutions division, in a statement to the press last year. “This decision was based on the high level of technology and experience on the site and is an investment in its future development.”
 
BASF has expanded its pipeline of solutions for agriculture significantly and, by 2028, will launch innovations with projected peak sales of more than €6 billion. The pipeline contains a wealth of chemical and biological crop protection products, seeds and traits, as well as digital solutions. This will further strengthen the company’s leading position in innovative and sustainable agriculture. This pipeline demonstrates tangible progress based on continuous investment in research and development, the integration of acquired businesses and strong partnerships. In 2019, BASF will spend around €900 million on R&D for agricultural solutions.
 
“We provide farmers with a full toolbox of innovative technologies, solutions and know-how, helping them develop their businesses successfully while addressing the demands of the food value chain,” said Markus Heldt, President of BASF’s Agricultural Solutions division. “We are actively steering our current and future portfolio towards more sustainable solutions . This enables us to develop highly-effective, innovative compounds that benefit farmers, society and the planet.”
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