113046-49-4

Upstream product

• 113045-95-7 ethyl 6-fluoro-4-oxo-1-phenyl-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate 
• 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 
• 84339-06-0 ethyl 7,6-difluoro-4-hydroxy-2-mercaptoquinoline-3-carboxylate 
• 113028-75-4 3,4-difluorophenyl isothiocyanate 
• 618-31-5 benzylidene dibromide 
• 144514-15-8 3,4-difluorophenyl dithiocarbamic acid triethylammonium 
• 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.

Substituted thiazetoquinoline-3-carboxylic acids and pharmaceutically acceptable salts thereof

Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: STR1 in which R1 is hydrogen, alkyl or substituted or unsubstituted phenyl; R2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R3 is hydrogen or substituted or unsubstituted alkyl; R4 and R5 are the same or different and are alkyl or hydroxyalkyl or R4 and R5 together with the nitrogen atom to which they are attached form an unsubstituted or substituted heterocyclic ring having the depicted nitrogen atom as the sole heteroatom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.