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Applications and constructions of benzazepine scaffolds in drug molecular design
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Bo HAN, Xin-yan PENG, Jian-qi LI, Qing-wei ZHANG*
Acta Pharmaceutica Sinica | 2022, 57(12) : 3564 - 3575
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Acta Pharmaceutica Sinica | 2022, 57(12): 3564-3575
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Applications and constructions of benzazepine scaffolds in drug molecular design
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Bo HAN, Xin-yan PENG, Jian-qi LI, Qing-wei ZHANG*
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  • Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai 201203, China
Published: 2022-12-12 doi: 10.16438/j.0513-4870.2022-0876
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Benzazepine is a kind of fused ring structure, which is composed of nitrogen-containing seven-membered ring and benzene ring. The introduction of benzazepine scaffolds into compounds can not only adjust the physicochemical properties, maintain or enhance the biological activities of the compounds, but also improve the pharmacokinetic properties, increase the brain permeability, and reduce the toxicity of hERG of the compounds, which is one of the privileged scaffolds for rational design and structural optimization of drug molecules. Benzazepine scaffolds can be constructed by different synthetic methods such as Dickmann condensation reaction, Mitsunobu reaction, Pictet-Spengler reaction, CMD reaction, multicomponent reactions (MCRs), metal catalysis reactions and asymmetric catalysis etc., which play an important role in enriching the structure diversity of drug molecules.

benzazepine  /  structure optimization  /  drug molecule  /  privileged scaffold  /  druggability
Bo HAN, Xin-yan PENG, Jian-qi LI, Qing-wei ZHANG. Applications and constructions of benzazepine scaffolds in drug molecular design[J]. Acta Pharmaceutica Sinica, 2022 , 57 (12) : 3564 -3575 . DOI: 10.16438/j.0513-4870.2022-0876
Year 2022 volume 57 Issue 12
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doi: 10.16438/j.0513-4870.2022-0876
  • Receive Date:2022-07-19
  • Online Date:2025-12-24
  • Published:2022-12-12
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  • Received:2022-07-19
  • Revised:2022-07-27
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    Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai 201203, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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