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Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
Design, Synthesis of Arylhydrazide and Thiazolamine Derivatives Based on Benzodioxole Scaffold as Potential
Yong Li1, Zebin Zhou1, Qing Zhang1
1State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine & School of Pharmaceutical Sciences, Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang 550004, People's Republic of China.
Abstract:
In an effort to develop novel fungicides characterized by high efficacy and low toxicity, this study designed and synthesized 62 benzodioxole-arylhydrazide and benzodioxole-thiazolamine derivatives. Their antifungal activities were evaluated against ten phytopathogenic fungi. The majority of arylhydrazide analogues exhibited significant inhibitory effects in vivo. Notably, compound 1e demonstrated the best broad-spectrum antifungal potency, with EC50 values ranging from 0.2 to 5.9 μg/mL. Further in vivo evaluation confirmed that 1e provided outstanding protective and curative effects against certain crop diseases. Preliminary mechanistic studies indicated that 1e exerted its antifungal effects by blocking spore germination, arresting germ tube elongation, and compromising fungal cell membrane integrity. Additionally, 1e displayed a favorable safety profile and promising plant-growth-modulating activity. These findings establish a solid foundation for the continued development of benzodioxole-derived compounds as novel botanical fungicides for agricultural protection.
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