Synthesis and Structure‐Activity Relationships of 3‐Arylisoquinolone Analogues as Highly Specific hCES2A Inhibitors

Mammalian carboxylesterases (CES) are key enzymes that participate in the hydrolytic metabolism of various endogenous and exogenous substrates. Human carboxylesterase 2A (hCES2A), mainly distributed in the small intestine and colon, plays a significant role in the hydrolysis of many drugs. In this s...

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Veröffentlicht in:	ChemMedChem 2021-01, Vol.16 (2), p.388-398
Hauptverfasser:	Zhao, Yitian, Xiong, Yuan, Dong, Sanfeng, Guan, Xiaoqing, Song, Yunqing, Yang, Yanqing, Zou, Kun, Li, Zhao, Zhang, Yong, Fang, Shengquan, Li, Bo, Zhu, Weiliang, Chen, Kaixian, Jia, Qi, Ge, Guangbo
Format:	Artikel
Sprache:	eng
Schlagworte:	3-arylisoquinolone Amides Bromine Carboxylesterase Cell permeability Colon hCES2A Inhibitors Intestine Intracellular Metabolism Molecular docking Small intestine specific structure−activity relationships Substrates
Online-Zugang:	Volltext
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