127625-07-4

Upstream product

• 133434-01-2 diethyl 2,3,4,6-tetrafluorobenzoylmalonate 
• 123016-54-6 ethyl 2-(2,3,4,6-tetrafluorobenzoyl)-3-cyclopropylacrylate 
• 123016-52-4 ethyl 2,3,4,6-tetrafluorobenzoylacetate 
• 123016-51-3 2,3,4,6-tetrafluorobenzoyl chloride 
• 32890-92-9 2,3,4,6-tetrafluorobenzoic acid 
• 1551-39-9 2,4,5,6-tetrafluoroisophthalic acid 
• 100-46-9 benzylamine 
• 123016-56-8 ethyl 5,7,8-trifluoro-1-cyclopropyl-1,4-dihydro-4-oxoquinoline-3-carboxylate 

Downstream Products

• 174312-99-3 5-Benzylamino-8-chloro-1-cyclopropyl-7-fluoro-6-nitro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Imidazo- and triazoloquinolones as antibacterial agents. Synthesis and structure-activity relationships

4,5-Disubstituted 6-cyclopropyl-6,9-dihydro-9-oxo-1H-imidazo- (30-32) and triazolo[4,5-f]quinoline-8-carboxylic acids (33-35) were synthesized starting from 5,6-diaminoquinolones 25. The imidazoquinolones 30-32 were equal or superior to the corresponding triazoloquinolone analogues 33-35 in in vitro antibacterial activity. As for the C-5 substituents, a fluorine atom was the most favorable of the three groups, H, F, and Cl. Among the compounds prepared, 4-(cyclic amino)-5-fluoro-imidazoquinolones 31a-d showed potent and well-balanced antibacterial activity against both gram-positive and gram- negative bacteria. Structure-activity relationships for the C-4 substituents (cyclic amino groups) were also examined in detail.