49818-48-6Relevant academic research and scientific papers
Benzo aza compound, preparation method and use thereof
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Paragraph 0099; 0100, (2017/08/22)
Belonging to the field of pharmaceutical chemistry, the invention relates to a benzoazepine compound, a preparation method and application thereof, in particular to the benzoazepine compound, its preparation method and application in the field of treatment of nervous system diseases, especially application in the field of drug addiction related to dopamine D1 and D3 receptors. The benzoazepine compound and pharmacologically acceptable inorganic or organic salts thereof have a structure shown as formula (I). Results of drug experiments carried out by the invention show that the benzoazepine compound and its pharmacologically acceptable inorganic or organic salts have high antagonistic activity on dopamine D1 and D3, can be used as drug leads for further development of dopamine receptor antagonists with good selectivity and high activity, and can be used as potential drugs for treatment of drug addiction by dopamine D1, D3 receptor antagonists. (formula (I)).
Functional reversal of (?)-Stepholidine analogues by replacement of benzazepine substructure using the ring-expansion strategy
Li, Wei,Zhang, Li,Xu, Lili,Yuan, Congmin,Du, Peng,Chen, Jiaojiao,Zhen, Xuechu,Fu, Wei
, p. 599 - 607 (2016/10/06)
(?)-Stepholidine is an active ingredient of the Chinese herb Stephania and naturally occurring tetrahydroprotoberberine alkaloid with mixed dopamine receptor D1 agonistic and dopamine receptor D2 antagonistic activities. In this work, a series of novel hexahydrobenzo[4,5]azepino [2,1-a]isoquinolines were designed and synthesized as ring-expanded analogues of (?)-Stepholidine. Initial pharmacological assays demonstrated that a benzazepine replacement was associated with significant increase in selectivity and functional reversal at dopamine receptor D1. Compound-(?)-15e (Ki?=?5.32?±?0.01?nm) is more potent than (?)-Stepholidine (Ki?=?13?nm) and was identified as a selective dopamine receptor D1 antagonist (IC50?=?0.14?μm). Moreover, molecular modeling suggested that (?)-15e might exert its dopamine receptor D1 antagonistic activities through interacting with the transmembrane helix 7 of dopamine receptor D1.
A facile synthesis of 1-alkyl-5-arylalkoxy-6-methoxy-3,4- dihydroisoquinolines
Yim, Heong-Seup,Kim, Ho-Kyun,Kim, Jeum-Jong,Kweon, Deok-Heon,Lee, Sang-Gyeong,Kim, Jung-Ho,Yoon, Yong-Jin
, p. 909 - 914 (2008/04/05)
(Chemical Equation Presented) 1-Alkyl-5-arylalkoxy-6-methoxy-3,4- dihydroisoquinolines were synthesized by the alkylation of 1-alkyl-5-hydroxy-6- methoxy-3,4-dihydroisoquinolines with arylalkyl halide in the presence of potassium carbonate. 1-Alkyl-5-hydroxy-6-methoxy-3,4-dihydroisoquinolines as key precursor prepared from o-vaniline via 6 steps.
