A series of some pyrazolo derivatives (1-2)(a-f) were synthesized and their urease inhibitory and tyrosinase inhibitory activities were evaluated. Among synthesized compounds, 2f, 2e, 1f, 2d, 1e, 2b, and 1d showed excellent activities (IC50) i.e. 11.73±0.28, 14.21±0.56, 15.37±0.89, 17.66±0.82, 18.64±0.19, 19.55±0.39, and 22.08±0.96 μM, respectively. According to tyrosinase assay results, compound 2f showed the good tyrosinase inhibitory activity i.e. 6.12±0.40 mM of IC50.