108138-16-5Relevant articles and documents
Method for efficiently and environmentally friendly preparing quinolones
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Paragraph 0024, (2019/01/05)
The invention discloses a method for efficiently and environmentally friendly preparing quinolones. Fluorobenzoylacetic acid ethyl ester, triethyl orthoformate and amine compounds are used as raw materials, and the quinolones are synthesized by maintainin
Effect of Lipophilicity at N-1 on Activity of Fluoroquinolones against Mycobacteria
Renau, Thomas E.,Sanchez, Joseph P.,Shapiro, Martin A.,Dever, Julie A.,Gracheck, Stephen J.,Domagala, John M.
, p. 2974 - 2977 (2007/10/02)
The dramatic increase in drug resistant Mycobacterium tuberculosis has caused a resurgence in research targeted toward these organisms.As part of a systematic study to optimize the quinolone antibacterials against mycobacteria, we have prepared a series of N-1-phenyl-substituted derivatives to explore the effect of increasing lipophilicity on potency at this position.The compounds, synthesized by the modification of a literature procedure, were evaluated for activity against Gram-negative and Gram-positive bacteria, Mycobacterium fortuitum and Mycobacterium smegmatis, and the results correlated with log P, pKa, and other attributes.The activity of the compounds against the rapidly growing, less hazardous organism M. fortuitum was used as a measure of M. tuberculosis activity.The results demonstrate that increasing lipophilic character by itself does not correlate with increased potency against mycobacteria.Rather, intrinsic activity against Gram-negative and/or Gram-positive bacteria is the governing factor for corresponding activity against mycobacteria.
Heterocycylic-substituted quinoline-carboxylic acids
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, (2008/06/13)
1-Substituted-6-fluoro-7-heterocyclic-1,4-dihydroquino-1-(or dihydronaphthyridin)-4-one carboxylic acids have antibacterial properties. The 7-heterocyclic group is a bicyclic group, one of the rings of which is saturated and the other ring of which is unsaturated.