Department of Microbiology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.
Arch Pharm (Weinheim). 2011 Mar;344(3):178-83. doi: 10.1002/ardp.201000013. Epub 2010 Dec 22.
A series of 5-nitroimidazole-based 1,3,4-thiadiazoles were prepared and tested for antibacterial activity against Helicobacter pylori. The anti-H. pylori activity of target compounds along with the commercially available antimicrobial metronidazole was evaluated by comparing the inhibition-zone diameters determined by the paper disc diffusion bioassay. From our bioassay results against 20 clinical isolates it is evident that piperazinyl, 4-methylpiperazinyl, 3-methylpiperazinyl, and 3,5-dimethylpiperazinyl analogs (6a, 6b, 6e, and 6f, respectively) and pyrrolidine derivative 7 had strong activity at 0.5 µg/disc (average of inhibition zone > 20 mm) while metronidazole had no activity at this dose. Compound 6f containing the 3,5-dimethylpiperazinyl moiety at the 2-position of the 5-(1-methyl-5-nitro-1H-imidazol-2-yl)-1,3,4-thiadiazole skeleton was the most potent compound tested at low concentrations.
一系列基于 5-硝基咪唑的 1,3,4-噻二唑类化合物被制备出来，并对其抗幽门螺杆菌的抗菌活性进行了测试。通过比较纸片扩散生物测定法确定的抑菌圈直径，评估了目标化合物以及市售抗菌药物甲硝唑的抗 H. pylori 活性。从我们对 20 株临床分离株的生物测定结果来看，哌嗪基、4-甲基哌嗪基、3-甲基哌嗪基和 3,5-二甲基哌嗪基类似物（6a、6b、6e 和 6f，分别）和吡咯烷衍生物 7 在 0.5 µg/disc 时具有很强的活性（平均抑菌圈>20mm），而甲硝唑在该剂量下没有活性。在 5-(1-甲基-5-硝基-1H-咪唑-2-基)-1,3,4-噻二唑骨架的 2-位含有 3,5-二甲基哌嗪基部分的化合物 6f 是在低浓度下测试的最有效化合物。
