Novel Isoniazid Embedded Triazole Derivatives: Synthesis, Antitubercular And Antimicrobial Activity Evaluation

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(2020)

引用 27|浏览3
暂无评分
摘要
In the present study, a series of new isoniazid embedded triazole derivatives have been synthesized. These compounds were evaluated for their in vitro antitubercular and antimicrobial activities. Among the screened compounds, six have exhibited potent antitubercular activity against Mycobacterium tuberculosis H37Rv strain with MIC value 0.78 mu g/mL, whereas, three compounds have displayed activity with MIC value ranging from 1.56 to 3.125 mu g/mL. The cytotoxicity of the active compounds was studied against RAW 264.7 cell line by MTT assay and no toxicity was observed even at 25 mu g/mL concentration. The five compounds have displayed good antimicrobial activities. Molecular docking have been performed against mycobacterial InhA enzyme to gain an insight into the plausible mechanism of action which could pave the way for our endeavor to identify potent antitubercular candidates. We believe that further optimization of these molecules may lead to potent antitubercular agents.
更多
查看译文
关键词
Isoniazid, 1, 2, 3-Triazole, Antitubercular activity, Antimicrobial activity, Cytotoxicity, Molecular docking, Click chemistry
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要