Synthesis and anti-Helicobacter pylori activity of 5-(nitroaryl)-1,3,4-thiadiazoles with certain sulfur containing alkyl side chain
作者:Alireza Foroumadi、Ardeshir Rineh、Saeed Emami、Farideh Siavoshi、Sadegh Massarrat、Fatemeh Safari、Saeed Rajabalian、Mehraban Falahati、Ensieh Lotfali、Abbas Shafiee
DOI:10.1016/j.bmcl.2008.04.033
日期:2008.6
A series of 5-(nitroaryl)-1,3,4-thiadiazoles bearing certain sulfur containing alkyl side chain similar to pendent residue in tinidazole molecule were synthesized and evaluated against Helicobacter pylori using disk diffusion method. The synthesized compounds were also evaluated for their antibacterial, antifungal and cytotoxic effects. Study of the structure-activity relationships of this series of
合成了一系列5-(硝基芳基)-1,3,4-噻二唑,它们带有类似于替硝唑分子中侧基的某些含硫烷基侧链,并使用圆盘扩散法对幽门螺杆菌进行了评估。还评估了合成的化合物的抗菌,抗真菌和细胞毒性作用。对这一系列化合物的构效关系的研究表明,硝基芳基单元的结构和1,3,4-噻二唑环2位上的侧基均显着影响抗H。幽门螺杆菌活动。尽管含有硝基噻吩系列中2- [2-(乙基磺酰基)乙硫基]侧链的化合物7a是针对幽门螺杆菌临床分离株测试的最有效的化合物,硝基咪唑6c和7c由于具有抗H的特性而被认为是更有前途的化合物。幽门螺杆菌活性除细胞毒性作用较小外。