Quinazolinone-based benzenesulfonamides with low toxicity and high affinity as monoamine oxidase-A inhibitors: Synthesis, biological evaluation and induced-fit docking studies

Bioorganic Chemistry(2022)

引用 17|浏览10
暂无评分
摘要
•Compounds 7 and 8 had IC50 values of 0.058 ± 0.002 and 0.094 ± 0.003 µM against MAO-A.•Compounds 7 and 8 were 105 and 65 times potent inhibitors than moclobemide towards MAO-A.•Compounds 7 (>1724 times) and 8 (>1063 times) more selective and reversible inhibitors of MAO-A rather than MAO-B.•Compounds 7 and 8 can be considered as non-toxic towards the SH-SY5Y cell line.•In silico docking simulations explained that structural water molecules to play a key role in the ligand-enzyme interactions.
更多
查看译文
关键词
Antidepressant,Monoamine oxidase,Quinazoline,Benzenesulfonamides,Docking
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