The photoswitchable ABAMIs for the future regulation of GWT1 in a spatiotemporal level

Photoswitchable bioactive molecules have attracted more attention and are widely used as photochromic ligands (PCLs) in both agrochemicals and pharmaceuticals. The glycosylphosphatidylinositol (GPI) acyltransferase GWT1 has been identified as a novel agricultural target of the 2‐aminopyridine fungicides. Herein, the GWT1‐targeted azobenzene‐aminopyridine derivatives ( ABAMIs ) were designed and synthesized to spatiotemporally regulate biological functions, which are promising tools in revealing the unclear antifungal mechanism. The maximal nine‐fold difference in activity was found between UV‐irradiated and unirradiated ABAMI1 against Botrytis cinerea ( B . cinerea ). This, in principle of concept, could realize the regulation of GWT1 functions. Furthermore, a three‐fold bioactivity difference against Sclerotinia sclerotiorum ( S . sclerotiorum ) was observed between the trans‐ and cis ‐ p F 4 ABAMI s that were sensitive to visible light. The ABAMIs were successfully developed as PCLs that were allowed to modulate fungicidal activity by light, providing innovative and powerful tools for understanding functional GWT1 and opening an avenue to the GWT1‐targeted pesticide discovery.