当前位置：
X-MOL 学术
›
Eur. J. Med. Chem.
›
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.)
Synthesis and antimycobacterial activity of thiazolidine-2,4-dione based derivatives with halogenbenzohydrazones and pyridinecarbohydrazones substituents.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-01-10 , DOI: 10.1016/j.ejmech.2020.112045 Nazar Trotsko 1 , Joanna Golus 2 , Paulina Kazimierczak 2 , Agata Paneth 1 , Agata Przekora 2 , Grazyna Ginalska 2 , Monika Wujec 1
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-01-10 , DOI: 10.1016/j.ejmech.2020.112045 Nazar Trotsko 1 , Joanna Golus 2 , Paulina Kazimierczak 2 , Agata Paneth 1 , Agata Przekora 2 , Grazyna Ginalska 2 , Monika Wujec 1
Affiliation
|
The two series of thiazolidine-2,4-dione (TZD) based hybrids with halogenbenzohydrazones and pyridinecarbohydrazones substituents were designed and synthesized. Target hydrazones were evaluated for their antimycobacterial activity by broth microdilution method with resazurin as an indicator of the metabolic activity of mycobacteria. Conducted studies revealed antimycobacterial activity in the concentration range of 1-512 μg/ml for 23 synthesized TZD-based derivatives. The highest antimycobacterial activity (MIC = 1 μg/ml) was demonstrated for the new group of compounds: TZD-based derivatives with pyridine-4-carbohydrazone substituent. Furthermore, all the tested compounds within this group were characterized by low cytotoxicity. On the basis of the results obtained, three compounds with the highest SI were selected. High effectiveness and safety of these synthesized derivatives makes them promising candidates as antimycobacterial agents.
中文翻译：
噻唑烷-2,4-二酮基衍生物的合成及其抗菌活性，该衍生物具有卤素苯并hydr和吡啶并咔唑取代基。
设计并合成了两个系列的基于噻唑烷-2,4-二酮（TZD）的具有卤素苯并hydr和吡啶并咔唑取代基的杂化物。通过肉汤微稀释法，以刃天青作为分枝杆菌代谢活性的指标，评估目标的抗分枝杆菌活性。进行的研究表明，对于23种基于TZD的合成衍生物，其分枝杆菌活性在1-512μg/ ml的范围内。对于新的化合物组，具有最高的抗分枝杆菌活性（MIC = 1μg/ ml）：具有吡啶-4-碳hydr取代基的TZD基衍生物。此外，该组中所有测试化合物的特征在于低细胞毒性。根据获得的结果，选择了三种SI最高的化合物。
更新日期：2020-01-10
中文翻译：
噻唑烷-2,4-二酮基衍生物的合成及其抗菌活性，该衍生物具有卤素苯并hydr和吡啶并咔唑取代基。
设计并合成了两个系列的基于噻唑烷-2,4-二酮（TZD）的具有卤素苯并hydr和吡啶并咔唑取代基的杂化物。通过肉汤微稀释法，以刃天青作为分枝杆菌代谢活性的指标，评估目标的抗分枝杆菌活性。进行的研究表明，对于23种基于TZD的合成衍生物，其分枝杆菌活性在1-512μg/ ml的范围内。对于新的化合物组，具有最高的抗分枝杆菌活性（MIC = 1μg/ ml）：具有吡啶-4-碳hydr取代基的TZD基衍生物。此外，该组中所有测试化合物的特征在于低细胞毒性。根据获得的结果，选择了三种SI最高的化合物。
京公网安备 11010802027423号