Design, synthesis, and biological evaluation of novel iso-flavones derivatives as H3R antagonists

被引：6

作者：

Xin, Jian ^{[1
,2
]}

Hu, Min ^{[3
]}

Liu, Qian ^{[3
]}

Zhang, Tian Tai ^{[3
]}

Wang, Dong Mei ^{[3
]}

Wu, Song ^{[3
]}

机构：

[1] Chinese Acad Med Sci, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China

[2] Peking Union Med Coll, Beijing 100050, Peoples R China

[3] Inner Mongolia Med Univ, Sch Pharm, Hohhot, Peoples R China

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2018年 / 33卷 / 01期

关键词：

H3R antagonist; iso-flavone; molecular docking; HISTAMINE H-3 RECEPTOR; INVERSE AGONIST; DISCOVERY; SIDE; BINDING; POTENT;

D O I：

10.1080/14756366.2018.1509212

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Histamine H-3 receptor (H3R), a kind of G-protein coupled receptor (GPCR), is expressed mainly in the central nervous system (CNS) and plays a vital role in homoeostatic control. This study describes the design and synthesis of a series of novel H3R antagonists based on the iso-flavone scaffold. The results of the bioactivity evaluation show that four compounds (1c, 2c, 2h, and 2o) possess significant H3R inhibitory activities. Molecular docking indicates that a salt bridge, pi-pi T-shape interactions, and hydrophobic interaction all contribute to the interaction between compound 2h and H3R.

引用

页码：1545 / 1553

页数：9

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