Suppr超能文献

新型喹唑啉基肼衍生物的设计、合成、分子建模及单胺氧化酶抑制活性筛选

Design, synthesis, molecular modelling and screening of monoamine oxidase inhibitory activities of novel quinazolyl hydrazine derivatives.

作者信息

Amer Adel, Hegazi Abdelrahman H, Alshekh Mohammed Khalil, Ahmed Hany E A, Soliman Saied M, Maniquet Antonin, Ramsay Rona R

机构信息

Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia.

Department of Chemistry, Faculty of Science, Alexandria University, Alexandria 21321, Egypt.

出版信息

R Soc Open Sci. 2020 Apr 22;7(4):200050. doi: 10.1098/rsos.200050. eCollection 2020 Apr.

Abstract

A new series of N'-substituted benzylidene-2-(4-oxo-2-phenyl-1,4-dihydroquinazolin-3(2H)-yl)acetohydrazide () has been synthesized, characterized by FT-IR, NMR spectroscopy and mass spectrometry and tested against human monoamine oxidase (MAO) A and B. Only (4-hydroxy-3-methoxybenzylidene) substituted compounds gave submicromolar inhibition of MAO-A and MAO-B. Changing the phenyl substituent to methyl on the unsaturated quinazoline ring () decreased inhibition, but a less flexible linker () resulted in selective micromolar inhibition of hMAO-B providing insight for ongoing design.

摘要

合成了一系列新型的N'-取代亚苄基-2-(4-氧代-2-苯基-1,4-二氢喹唑啉-3(2H)-基)乙酰肼(),通过傅里叶变换红外光谱、核磁共振光谱和质谱对其进行了表征,并针对人单胺氧化酶(MAO)A和B进行了测试。只有(4-羟基-3-甲氧基亚苄基)取代的化合物对MAO-A和MAO-B表现出亚微摩尔级别的抑制作用。将不饱和喹唑啉环上的苯基取代基换成甲基()会降低抑制作用,但一个柔性较小的连接基()导致对人单胺氧化酶B产生选择性微摩尔级抑制作用,这为正在进行的设计提供了思路。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8852/7211837/aa40865597f4/rsos200050-g1.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验