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.
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.
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。
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