Drug discovery and development is a time-consuming, interdisciplinary and expensive process. Advances in computational procedures have empowered in silico routines, and specifically structure based drug design technique, to accelerate new target choice through the recognizable proof of hits for the improvement of lead compounds in the medication discovery process. Hence, the present work aims to identify the potent 1,2,3 triazole appended piperazine compounds for synthesis. In-silico design of novel analogues were carried out using Auto Dock Vina,Swiss ADME software was used to analyse ‗Lipinski Rule of Five‘ and drug likeness properties. Ten derivatives which obeyed the rule of five and having desired physio-chemical properties and highest docking score were synthesized The synthesis has been carried out in two step process to determine their Anti-microbial and Invitro Anti-cancer activity.