Design And Synthesis Of New Indanol-1,2,3-Triazole Derivatives As Potent Antitubercular And Antimicrobial Agents

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(2020)

引用 24|浏览4
暂无评分
摘要
In a search of new antitubercular agents, herein we have reported a series of new thirty-two indanol-1,2,3-triazole derivatives. The synthesized compounds were screened for their in vitro antitubercular and antimicrobial activities. Among the screened compounds, most of the compounds have displayed good antitubercular activity against Mycobacterium tuberculosis H37Rv. The compound 5g has been identified as potent antitubercular agent with MIC value 1.56 p.M. The most active compounds of the series were further studied for their cytotoxicity against HEK 293 cells using MIT assay and found to be nontoxic. In addition, ten compounds were shown good antimicrobial activities against both antibacterial and antifungal pathogens. A molecular docking study against Mycobacterial enoyl-ACP-reductase (InhA) was performed to gain an insight into the molecular mechanism of antitubercular action. The pharmacokinetic parameters of these compounds were studied and displayed acceptable drug-likeness score.
更多
查看译文
关键词
1,2,3-Triazoles, Antitubercular activity, Antimicrobial activity, Click chemistry, Molecular docking study, ADME prediction
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