Synthesis and antibacterial activity of 7-(4-acylamino-thiocarbamoyl-1-piperazinyl) fluoroquinolone analogues in vitro.
- Author:
Ling-bo QU
1
;
Meng-chao TIAN
;
Sen-xiang CHENG
;
Rong-feng CHEN
Author Information
- Publication Type:Journal Article
- MeSH: Anti-Infective Agents; chemical synthesis; chemistry; pharmacology; Bacillus subtilis; drug effects; Ciprofloxacin; chemistry; pharmacology; Combinatorial Chemistry Techniques; methods; Escherichia coli; drug effects; Fluoroquinolones; chemical synthesis; chemistry; pharmacology; Microbial Sensitivity Tests; Molecular Structure; Norfloxacin; chemistry; pharmacology
- From: Acta Pharmaceutica Sinica 2003;38(4):264-267
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo synthesize new fluoroquinolone analogues as antibacterial compounds.
METHODS AND RESULTSBy 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.
CONCLUSIONAntibacterial activities of the new compounds were evaluated in vitro compared with norflorxacin. Compounds 5, 7, 10 and 12 showed antibacterial activities.
