Synthesis and antibacterial activity of 7-(4-acylamino-thiocarbamoyl-1-piperazinyl) fluoroquinolone analogues in vitro / 药学学报

ABSTRACT

<p><b>AIM</b>To synthesize new fluoroquinolone analogues as antibacterial compounds.</p><p><b>METHODS AND RESULTS</b>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.</p><p><b>CONCLUSION</b>Antibacterial activities of the new compounds were evaluated in vitro compared with norflorxacin. Compounds 5, 7, 10 and 12 showed antibacterial activities.</p>