108115-67-9

Upstream product

• 367-25-9 2,4-difluorophenylamine 
• 98349-24-7 ethyl 2,4,5-trifluorobenzoylacetate 
• 122-51-0 orthoformic acid triethyl ester 
• 446-17-3 2,4,5-trifluorobenzoic acid 
• 367-23-7 1,2,4-trifluorobenzene 
• 88419-56-1 2,4,5-trifluorobenzoyl chloride 
• 129322-83-4 2',4',5'-trifluoroacetophenone 

Downstream Products

• 108138-17-6 6,7-difluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid ethyl ester 
• 108138-27-8 A 57531 
• 103995-01-3 6,7-difluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid 
• 130982-85-3 (S)-(-)-temafloxacin 
• 130982-86-4 (R)-(+)-temafloxacin 

Relevant academic research and scientific papers

Effect of Lipophilicity at N-1 on Activity of Fluoroquinolones against Mycobacteria

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.

Synthesis, Antibacterial Activities, and Pharmacological Properties of Enantiomers of Temafloxacin Hydrochloride

Temafloxacin hydrochloride is a potent member of the 4-pyridone-3-carboxylic acid class of antibacterial agents and is currently under clinical development as a broad-spectrum antimicrobial agent.It is a racemate having a chiral center at the C3 of the 7-piperazin-1-yl group.The two enantiomers were synthesized and tested for their antibacterial activities.Although no difference in in vitro antibacterial activities was observed, a minor difference in in vivo antibacterial activities was observed.However, they both exhibited similar pharmacological profiles.