Design,synthesis, and biological evaluation of novel iso-flavones derivatives as H3R antagonists |
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| Authors: | Jian Xin Min Hu Qian Liu Tian Tai Zhang |
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| Affiliation: | 1. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China;2. School of Pharmacy, Inner Mongolia Medical University, Hohhot, China |
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| Abstract: | Histamine H3 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, π–π T-shape interactions, and hydrophobic interaction all contribute to the interaction between compound 2h and H3R. |
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| Keywords: | H3R antagonist iso-flavone molecular docking |
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