Wallace Michael D, Debowski Aleksandra W, Sukhoverkov Kirill V, Mylne Joshua S, Stubbs Keith A
School of Molecular Sciences The University of Western Australia Crawley WA Australia.
School of Biomedical Sciences The University of Western Australia Crawley WA Australia.
Plant Direct. 2021 Sep 14;5(9):e348. doi: 10.1002/pld3.348. eCollection 2021 Sep.
Development of herbicides with novel modes of action is crucial for weed control and to hinder herbicide resistance. An attractive novel herbicidal target is plant DNA gyrase, which has been demonstrated to be effectively inhibited by the known antimicrobial ciprofloxacin. Despite this good herbicidal activity, ciprofloxacin is not suitable as a herbicide due to its antimicrobial activity; therefore, a diverse library of analogues was analyzed to gain insight into the aspects required for herbicidal activity. This analysis revealed that significant structural modifications were tolerated and that the fluoride at C-6 and a cyclic amino group at C-7 were not crucial for herbicidal activity. The analysis also revealed that these modifications also affected the antibacterial activity with one compound demonstrating good herbicidal activity and weak antibacterial activity, against both Gram-positive and Gram-negative bacteria.
开发具有新型作用模式的除草剂对于杂草控制和阻碍除草剂抗性至关重要。一种有吸引力的新型除草靶标是植物DNA促旋酶,已证明它能被已知的抗菌药物环丙沙星有效抑制。尽管环丙沙星具有良好的除草活性,但由于其抗菌活性,它不适合用作除草剂;因此,分析了一个多样化的类似物文库,以深入了解除草活性所需的方面。该分析表明,可耐受显著的结构修饰,且C-6位的氟和C-7位的环氨基对除草活性并非至关重要。分析还表明,这些修饰也影响抗菌活性,其中一种化合物对革兰氏阳性菌和革兰氏阴性菌均表现出良好的除草活性和较弱的抗菌活性。