[Synthesis and antibacterial activity of 7-(4-acylamino-thiocarbamoyl-1-piperazinyl) fluoroquinolone analogues in vitro].
OBJECTIVE
To synthesize new fluoroquinolone analogues as antibacterial compounds.


RESULTS
By reaction of acryl chloride(chloro-carbonic ester) with sodium sulfocyanate, acyl isosulfocyanic ester were easily obtained. Twelve 7-(4-acylamino-thiocarbamoyl-1-piperazinyl) fluoroquinolone analogues (1-12) were synthesized through modifying the 7-piperazine of norflorxacin and ciprofloxacin with isosulfocyanic ester synthesized above. The structures of synthesized compounds were characterized by 1HNMR, IR and elemental analysis.


CONCLUSIONS
Antibacterial activities of the new compounds were evaluated in vitro compared with norflorxacin. Compounds 5, 7, 10 and 12 showed antibacterial activities.
Qu
Ling-bo
LB
Department of Chemistry, Zhengzhou University, Zhengzou 450052, China. Lbqu@371.net
Tian
Meng-chao
MC
Cheng
Sen-xiang
SX
Chen
Rong-feng
RF
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001412:Bacillus subtilis / Q000187:drug effects; D002939:Ciprofloxacin / Q000737:chemistry / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D004926:Escherichia coli / Q000187:drug effects; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009643:Norfloxacin / Q000737:chemistry / Q000494:pharmacology
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D002939:Ciprofloxacin; D009643:Norfloxacin