Abstract: AIM: To screen the hypoglycemic activity of diferent sulphonylureas derivative ligand and their metal complexes. METHODS: The mice were administered intragastrically, the blood samples were obtained from tail vein. The serum glucose levels were determined by glucose-oxidase-peroxidase (GOD-PAP) method. The hypoglycemic activities were analyzed by the mean of tolbutamide as a positive control drug, and its mechanism and structure-activity relationship between chemical structure and hypoglycemic activity were studied. RESUITS: The results showed that ZnL₂·2H₂O, NdL₃·2H₂O, SmL₃·2H₂O, Zn(HL')₂·2NO₃, Eu(HL')₃·3NO₃, HL and HL' all reduced the blood sugar in normal mice, while EuL₃·2H₂O, Nd(HL')₃·3NO₃ and Sm(HL')₃·3NO₃ had no obvious hypoglycemic activity. CONCLUSION: The hypoglycemic activity of HL is stronger than that of tolbutamide in normal mice at 2 h, indicating that when the first substituent of tosylurea is the alicyclic group (cyclohexyl), its hypoglycemic activity may be higher than the straight-chain lipid group (butyl), and much higher than the heterocyclic group (4-antipyrine).

Key words: 1-cyclohexyl-3-tosylurea, 1-(4-antipyrine)-3-tosylurea, Sulphonylureas derivative metal complexes, Hypoglycemic activity, Structure-activity relationship