113045-94-6

Upstream product

• 618-31-5 benzylidene dibromide 
• 3863-11-4 3,4-difluoroaniline 
• 113028-76-5 diethyl<<(3,4-difluorophenyl)amino><(methoxymethyl)-thio>methylene>malonate 
• 113028-77-6 ethyl 6,7-difluoro-4-hydroxy-2-<(methoxymethyl)thio>-quinoline-3-carboxylate 
• 144514-15-8 3,4-difluorophenyl dithiocarbamic acid triethylammonium 
• 84339-06-0 ethyl 7,6-difluoro-4-hydroxy-2-mercaptoquinoline-3-carboxylate 
• 113028-75-4 3,4-difluorophenyl isothiocyanate 
• 109-01-3 1-methyl-piperazine 
• 144514-21-6 6,7-Difluoro-4-oxo-1-phenyl-4H-2-thia-8b-aza-cyclobuta[a]naphthalene-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

STUDIES ON PYRIDONECARBOXYLIC ACIDS. 1. SYNTHESIS AND ANTIBACTERIAL EVALUATION OF 7-SUBSTITUTED-6-HALO-4-OXO-4H-THIAZETOQUINOLINE-3-CARBOXYLIC ACIDS

A series of thiazetoquinoline-3-carboxylic acids and their esters were prepared and evaluated for antibacterial activity.The derivatives with a hydrogen or methyl group at C-1, fluorine at C-6, and piperazinyl or 4-methyl-1-piperazinyl group at C-7 showed superior in vitro antibacterial activity, and the derivatives with 4-methyl-1-piperazinyl group at C-7 had potent in vivo activity.Compound 29a (NM394) showed excellent in vitro antibacterial activity and low toxicity but poor absorption from the gastrointestinal tract.Compound 29ee (NM441), an N- derivative of 29a, was found to possess a favorable pharmacokinetic profile and oral activity superior to that of ciprofloxacin in experimental animals.