[Structure and anti-M. leprae activity relationships of new quinolones].
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.
Gidoh
Masaichi
M
Leprosy Research Center, National Institute of Infectious Diseases, 4-2-1, Aoba-cho, Higashimurayama-shi, Tokyo 189-0002, Japan. m-gidoh@nih.go.jp
D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000494:pharmacology*; D015169:Colony Count, Microbial; D024881:Drug Resistance, Bacterial; D005260:Female; D024841:Fluoroquinolones / Q000737:chemistry* / Q000494:pharmacology*; D007918:Leprosy / Q000382:microbiology; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009166:Mycobacterium leprae / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones