7-（4-酰氨基硫代甲酰基-1-哌嗪基）喹诺酮类化合物的合成及其体外抗菌活性7-（4-酰氨基硫代甲酰基-1-哌嗪基）喹诺酮类化合物的合成及其体外抗菌活性

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

摘要: 目的合成新型含氟喹诺酮类抗菌化合物。方法与结果将酰氯与硫氰酸钠反应并经分子内热重排生成的酰基硫代异氰酸酯对诺氟沙星、环丙沙星的7-位哌嗪基进行修饰，合成了12个7-(4-酰氨基硫代甲酰基-1-哌嗪基)喹诺酮类似物，利用核磁共振、元素分析和红外光谱进行了结构确认。结论初步体外抗菌活性测试结果表明，所合成的化合物有一定的抗菌活性，且高于对照药诺氟沙星。

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.