Design, Synthesis, in vitro and in silico Characterization of 2‐Quinolone‐L‐alaninate‐1,2,3‐triazoles as Antimicrobial Agents

• DOI: 10.1002/cmdc.202100714
• Publication Date: 2022-01-03T03:05:48Z
• Authors: Oussama Moussaoui; Rajendra Bhadane; Riham Sghyar; Janez Ilaš; El Mestafa El Had...; Said Chakroune; Outi M. H. Salo‐Ahen
• Keywords: Quinolone; Moiety

Due to the ever-increasing antimicrobial resistance there is an urgent need continuously design and develop novel agents. Inspired by broad antibacterial activities of various heterocyclic compounds such as 2-quinolone derivatives, we designed synthesized new methyl-(2-oxo-1,2-dihydroquinolin-4-yl)-L-alaninate-1,2,3-triazole derivatives via 1,3-dipolar cycloaddition reaction 1-propargyl-2-quinolone-L-alaninate with appropriate azide groups. The were obtained in good yield ranging from 75 80 %. chemical structures these hybrid molecules determined spectroscopic methods activity was investigated against both bacterial fungal strains. tested showed significant weak moderate antifungal activity. Despite evident similarity quinolone moiety our fluoroquinolones, do not function inhibiting DNA gyrase. Computational characterization shows that they have attractive physicochemical pharmacokinetic properties could serve templates for developing potential agents clinical use.