期刊论文详细信息
Bulletin of the Korean chemical society
Synthesis of Tetracyclic Pyrido[2,3-b]azepine Derivatives as Analogues of Mirtazapine via N-Acyliminium Ion Cyclization
Changbae Jin1  Yong Sup Lee1  Jae Yeol Lee1  Sook Ja Lee1  Hokoon Park1  Sung Hun Bang1  Yun Seon Song1 
关键词: Homooxacalix[4]arene;    Conformation;    Crystal structure;   
DOI  :  
学科分类:化学(综合)
来源: Korean Chemical Society
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【 摘 要 】

Tetracyclic pyrido[2,3-b]azepine derivatives 4a-d and 4f as analogues of mirtazapine were synthesized via N-acyliminium ion cyclization by using aromatic rings such as benzene and thiophene ring as a �?-nucleophile,and evaluated for the binding affinity for �?2-adrenoceptor. Among tested compounds, 2,3,9,13b-tetrahydro-1H-benzo[f]pyrrolo[2,1-a]pyrido[2,3-c]azepine (4a) was the most potent (Ki = 0.26 レM) but showed about 3-fold less binding affinity than mirtazapine (Ki = 0.08 レM) for a2-adrenoceptor.

【 授权许可】

Unknown   

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