In this work we describe a simple method to synthesis of some novel piperidine derivative. The Structures of the newly synthesized compound were supported by means of FTIR, CHN elemental analysis, and NMR (1H, 13C) spectroscopic analysis. The synthesized compounds were evaluated for their in vitro antibacterial activity against Escherichia coli, Staphylococcus aureus, Aspergillus niger and Mucor. The inhibition zones were measured, expressed in mm, and the minimum inhibitory concentration (MIC) is reported in μg/mL. The results show that compound have a significant antimicrobial activity with the highest MIC value against all tested bacteria. The comparative molecular docking studies revealed better insights into binding mechanisms