Qu Ling-bo, Tian Meng-chao, Cheng Sen-xiang, Chen Rong-feng
Department of Chemistry, Zhengzhou University, Zhengzou 450052, China.
Yao Xue Xue Bao. 2003 Apr;38(4):264-7.
To synthesize new fluoroquinolone analogues as antibacterial compounds.
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.
Antibacterial activities of the new compounds were evaluated in vitro compared with norflorxacin. Compounds 5, 7, 10 and 12 showed antibacterial activities.
合成新型氟喹诺酮类似物作为抗菌化合物。
通过丙烯酰氯（氯代碳酸酯）与硫氰酸钠反应，可轻松得到异硫氰酸酯酰基。通过用上述合成的异硫氰酸酯修饰诺氟沙星和环丙沙星的7 - 哌嗪，合成了12种7 - （4 - 酰氨基 - 硫代甲酰基 - 1 - 哌嗪基）氟喹诺酮类似物（1 - 12）。合成化合物的结构通过1HNMR、IR和元素分析进行表征。
与诺氟沙星相比，对新化合物的抗菌活性进行了体外评估。化合物5、7、10和12显示出抗菌活性。
