Kang, Tao published the artcileDesign, Synthesis, and SAR of Novel 1,3-Disubstituted Imidazolidine or Hexahydropyrimidine Derivatives as Herbicide Safeners, Related Products of chlorides-buliding-blocks, the publication is Journal of Agricultural and Food Chemistry (2021), 69(1), 45-54, database is CAplus and MEDLINE.
Herbicide safeners enhance herbicide detoxification in crops without reducing their herbicidal efficacy against target weeds. To alleviate maize injury caused by the sulfonylurea herbicide nicosulfuron, a series of 1,3-disubstituted imidazolidine or hexahydropyrimidine derivatives were rationally designed via bioisosterism and active subunit combinations. Thirty novel compounds were synthesized using an efficient one-pot method and low-cost raw materials and characterized by IR, 1H NMR, 13C NMR, and high-resolution mass spectrometer (HRMS). Bioactivity and structure-activity relationship (SAR) were evaluated for herbicide safeners tested against nicosulfuron injury. Most of the compounds effectively protected sensitive maize against nicosulfuron damage. The parent skeletons and substituents of the target compounds both substantially influenced their safener activity. Compound (I) exhibited superior bioactivity compared to the safener isoxadifen-Et. Mol. docking simulations disclosed that compound I competed with nicosulfuron for the acetolactate synthase active site and demonstrated that this is the protective mechanism of safeners. The target compound I presented with strong herbicide safener activity in maize and is, therefore, a potential candidate for the development of a novel herbicide safener.
Journal of Agricultural and Food Chemistry published new progress about 3919-74-2. 3919-74-2 belongs to chlorides-buliding-blocks, auxiliary class Isoxazole,Fluoride,Chloride,Carboxylic acid,Benzene, name is 3-(2-Chloro-6-fluorophenyl)-5-methylisoxazole-4-carboxylic acid, and the molecular formula is C11H7ClFNO3, Related Products of chlorides-buliding-blocks.
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