01321nas a2200289 4500000000100000008004100001260001300042653002500055653001200080653002600092653002800118653003100146653001100177653002100188653001200209653000900221653002400230653001500254653002500269653003600294100001200330245007700342300001000419490000700429520058100436022001401017 2009 d c2009 Feb10aAdministration, Oral10aAnimals10aAnti-Bacterial Agents10aColony Count, Microbial10aDrug Resistance, Bacterial10aFemale10aFluoroquinolones10aleprosy10aMice10aMice, Inbred BALB C10aMice, Nude10aMycobacterium leprae10aStructure-Activity Relationship1 aGidoh M00a[Structure and anti-M. leprae activity relationships of new quinolones]. a17-230 v783 a

Due to the emergence of drug resistant M. leprae, there is a need to look for new drugs for the treatment of leprosy. We evaluated the effectiveness of new quinolones in vitro as well as in vivo. The in vitro and in vivo results suggested that a cyclopropyl group at the 1-position, COOH at the 3-position, OH at the 4-position, NH2 or OH-substitutions at the 5-position, F at the 6-position, 5- and 6-membered rings at the 7-position, halogen (F or Cl) or OCH3 at the 8-position of the quinolone core structure remarkably enhance anti-M. leprae activities of the drug.

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