当前位置：
X-MOL 学术
›
Chem. Bio. Drug Des.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Preparation and biological evaluation of metronidazole derivatives with monoterpenes and eugenol
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-08-05 , DOI: 10.1111/cbdd.13366 Majdi M. Bkhaitan 1 , Mohammed Alarjah 1 , Agha Zeeshan Mirza 2 , Ashraf N. Abdalla 3 , Hamdi M. El-Said 4 , Hani S. Faidah 4
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-08-05 , DOI: 10.1111/cbdd.13366 Majdi M. Bkhaitan 1 , Mohammed Alarjah 1 , Agha Zeeshan Mirza 2 , Ashraf N. Abdalla 3 , Hamdi M. El-Said 4 , Hani S. Faidah 4
Affiliation
|
Two series of metronidazole derivatives (ester derivatives and ether derivatives) were prepared reacting metronidazole and its acetic acid oxidized form with menthol, thymol, carvacrol, and eugenol. Both series of compounds were tested in vitro against two strains of Helicobacter pylori (the ATCC 26695 and P12), and one strain of Clostridium (Clostridium perfringens). Most of the prepared compounds showed biological activity against the targeted bacteria. Compound 11 was highly active against all tested bacterial strains, especially against P12 with IC50 0.0011 μM/ml. Compound 6 was highly active against C. perfringens with MIC 0.0094 nM/ml. Viability test was conducted for compound 11 to test its selectivity for normal human fetal lung fibroblasts (MRC5), and it was found to be non‐toxic with IC50 more than 50 μM/ml.
中文翻译：
单萜类和丁香酚对甲硝唑衍生物的制备及生物学评价
制备了两个系列的甲硝唑衍生物（酯衍生物和醚衍生物），使甲硝唑及其乙酸氧化形式与薄荷醇，百里酚，香芹酚和丁香酚反应。这两个系列的化合物都针对两种幽门螺杆菌（ATCC 26695和P12）和一种梭菌（Clostridium perfringens）进行了体外测试。大多数制备的化合物显示出针对靶细菌的生物活性。化合物11对所有测试的细菌菌株均具有很高的活性，尤其是对P12的IC 50为0.0011μM/ ml。化合物6对产气荚膜梭菌具有高活性MIC 0.0094 nM / ml。对化合物11进行了活力测试，以测试其对正常人胎儿肺成纤维细胞（MRC5）的选择性，发现IC 50大于50μM/ ml时无毒。
更新日期：2018-08-05
中文翻译：
单萜类和丁香酚对甲硝唑衍生物的制备及生物学评价
制备了两个系列的甲硝唑衍生物（酯衍生物和醚衍生物），使甲硝唑及其乙酸氧化形式与薄荷醇，百里酚，香芹酚和丁香酚反应。这两个系列的化合物都针对两种幽门螺杆菌（ATCC 26695和P12）和一种梭菌（Clostridium perfringens）进行了体外测试。大多数制备的化合物显示出针对靶细菌的生物活性。化合物11对所有测试的细菌菌株均具有很高的活性，尤其是对P12的IC 50为0.0011μM/ ml。化合物6对产气荚膜梭菌具有高活性MIC 0.0094 nM / ml。对化合物11进行了活力测试，以测试其对正常人胎儿肺成纤维细胞（MRC5）的选择性，发现IC 50大于50μM/ ml时无毒。
京公网安备 11010802027423号