Chalcones have a distinctive 1,3-diaryl propenone skeleton and exert numerous biological effects. Previously we synthesized (1a-23) bichalcones through the piperazine Mannich base linkage with different substitution on the both ring-B of the chalcone moieties. These compounds were subjected into the inhibitory effects on Formyl-Met-Leu-Phe (FMLP) and cytochalasin B (CB) stimulated O2 •− generation and elastase release in human neutrophils. Among the tested compounds, 3-23 were exhibited potent elastase release inhibitory effects in activated human neutrophils with the IC50 values ranges from 4.98 μM to 50.87 μM