A series of 5-chloro-1-(piperidin-4-yl)-1H-benzo[d]imidazole-2(3H)-one derivatives have been synthesized and characterized by various spectroscopic techniques including FTIR, mass and 1H NMR. In current study, we have followed standard methods for the synthesis of novel molecules, docking and screening against mycobacterium species. The compounds were docked against 2Q1Y protein by using MCULE software and screened them by MABA. Out of sixteen synthesized molecules, two molecules i.e. DSR-14 and DSR-9 had shown good antitubercular activity.