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Syntheses of quinolone hydrochloride enantiomers from synthons (R)- and (S)-2-methylpiperazine
Authors:Liu Bo  Yang Chun-Hao  Xu Guang-Yu  Zhu Yong-Hong  Cui Jing-Rong  Wu Xi-Han  Xie Yu-Yuan
Institution:State Key Laboratory of Drug Research, Shanghai Institute of Meteria Medica, SIBS, Chinese Academy of Sciences, Graduate School of the CAS, 555 Zuchongzhi Road, Shanghai 201203, PR China.
Abstract: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.
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