The hybrid congener 3 derived from hydroxychalcone and pharmacophore oxypropanolamine for adrenergic receptor, along with its enantiomers 9a and 9b were selected from a series of compounds for detailed studies of their antidiabetic profile in sucrose-challenged, low-dosed, streptozotocin-induced diabetic rats and in db/db mice, and antidyslipidaemic profile in high fat diet-induced dyslipidaemic hamsters. The test compounds exhibited significant and consistent antidiabetic and antidyslipidaemic activities in the above models.