Methyloxime-substituted aminopyrrolidine: a new surrogate for 7-basic group of quinolone.
Novel fluoroquinolones containing oxime functionalized aminopyrrolidines have been synthesized. They were found to possess potent antibacterial activities against both Gram-negative and Gram-positive organisms, including methicillin resistant Staphylococcus aureus (MRSA). Among these compounds, LB20277 (compound 12) showed the most favorable in vivo efficacy and pharmacokinetic profile in animals. Based on these promising results, LB20277 was selected as a candidate for further evaluation.
Hong
C Y
CY
Biotech Research Institute, Tae-Jon, Korea.
Kim
Y K
YK
Lee
Y H
YH
Kwak
J H
JH
D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D004285:Dogs; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006860:Hydrogen Bonding; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D009643:Norfloxacin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D010091:Oximes / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D013816:Thermodynamics
D000890:Anti-Infective Agents; C116731:LB 20277; D010091:Oximes; D009643:Norfloxacin