[Synthesis and antibacterial activity of 7-(4-acylamino-thiocarbamoyl-1-piperazinyl) fluoroquinolone analogues in vitro]

Yao Xue Xue Bao. 2003 Apr;38(4):264-7.
[Article in Chinese]

Abstract

Aim: To synthesize new fluoroquinolone analogues as antibacterial compounds.

Methods and 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.

Conclusion: Antibacterial activities of the new compounds were evaluated in vitro compared with norflorxacin. Compounds 5, 7, 10 and 12 showed antibacterial activities.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology
  • Bacillus subtilis / drug effects
  • Ciprofloxacin / chemistry
  • Ciprofloxacin / pharmacology
  • Combinatorial Chemistry Techniques / methods
  • Escherichia coli / drug effects
  • Fluoroquinolones / chemical synthesis*
  • Fluoroquinolones / chemistry
  • Fluoroquinolones / pharmacology
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Norfloxacin / chemistry
  • Norfloxacin / pharmacology

Substances

  • Anti-Infective Agents
  • Fluoroquinolones
  • Ciprofloxacin
  • Norfloxacin