Design and Synthesis of Novel Coumarin-Piperazine Derivatives as Potential Antimicrobial Agents

Coumarin piperazine acetamide analogues have shown great potential as drug candidates due to their wide range of biological activities. A series of novel coumarin-piperazine derivatives were synthesized and performed the in vitro antibacterial activity and ADME profiling. Compounds MS1, MS2, MS5 and MS6 exhibited docking scores higher than the standard ranging from -8.6 to -7.6 Kcal mol-1. Compound MS6 showed the best zone of inhibition, measuring 17 mm at 150 µg/mL against Staphylococcus epidermidis. Molecular docking and in vitro study of compound suggest that the presence of halogen on the aromatic ring, attached to piperazine might responsible for a good antibacterial potential. ADME profiling of the synthesized compounds showed the log S ESOL value between -2.39 to -4.52, number of H bond acceptors between 4-5, No. of H bond donors 1, high GIT absorption and adhered to the Lipinski, Ghose and Veber drug-likeness rules.