Synthesis and biological evaluation of pentacyclic triterpenoid derivatives as potential novel antibacterial agents

• Novel triterpene derivatives with aromatic ring were designed and synthesized. 18 ? -Glycyrrhetinic acid exhibited excellent MIC MBC of Staphylococcus. Representative compounds displayed stable antibacterial effect in killing kinetic studies. Molecular docking was performed rationalize the observed activity. Candidate compound 33 showed reasonable DMPK profiles low cytotoxicity. A series ursolic (UA), oleanolic (OA) -glycyrrhetinic (GA) synthesized by introducing a range substituted side-chains at C-2 position after hydroxyl group C-3 oxidized. Their activities evaluated vitro against panel four Staphylococcus spp. The results revealed that introduction GA led to discovery potent triterpenoid for inhibition both drug sensitive resistant S. aureus , while other two UA OA no significant activity even high concentrations. In particular, derivative good potency all (MIC = 1.25–5 ?mol/L) acceptable pharmacokinetics properties cytotoxicity . also using DNA gyrase This has strong potential development new type agent.