A new series derived from 4‐(2‐chloroacetyl)‐1,2‐dihydro‐2,3‐dimethyl‐1‐phenylpyrazol‐5‐one was synthesized and characterized, and its pharmacological activity toward α‐glucosidase and α‐amylase enzyme inhibition was screened. Moreover, molecular docking studies were conducted to support the findings.