Syntheses of quinolone hydrochloride enantiomers from synthons (R)- and (S)-2-methylpiperazine

A series of R and S enantiomers of 7-(3-methylpiperazin-1-yl) quinolone derivatives were synthesized from (R)- and (S)-tert-butyl 2-methylpiperazine-1-carboxylate and tested for their antibacterial activities on 14 kinds of bacteria. Although no distinct difference in in vitro antibacterial activities was observed, 2–64-fold difference between R and S enantiomers was observed in approximately 52% of cases.

A series of chiral quinolone hydrochloride was synthesized from synthons (R)- and (S)-2-methylpiperazine in high yield and tested for their antibacterial activity to explore the steric influence on biological activities.Figure optionsDownload as PowerPoint slide