Abstract: The present invention relates to an anisomycin derivative represented by general formula (I) or pharmaceutically acceptable salts, solvates and stereoisomers thereof. According to the present invention, it is found that anisomycin and derivatives thereof have the effect of promoting insulin secretion under high blood sugar concentrations, and can treat diabetes and prevent the occurrence of hypoglycemia. It is found, by studying its mechanism of action, that the anisomycin derivative is highly related to GLP-1R, indicating that the anisomycin derivative is a small molecule GLP-1R agonist, which can effectively treat a variety of GLP-1R-mediated diseases including obesity and diabetes, and has good commercial application prospects and scientific research value.