913613-99-7Relevant articles and documents
Preparation method of amide-like derivative and intermediate thereof
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, (2020/07/12)
The invention discloses a preparation method of an amide-like derivative and an intermediate thereof. The invention provides a preparation method of a compound as shown in a formula VI and an intermediate thereof, the compound as shown in the formula VI c
Isoquinolinone derivatives as potent CNS multi-receptor D2/5-HT1A/5-HT2A/5-HT6/5-HT7 agents: Synthesis and pharmacological evaluation
Cao, Xudong,Chen, Yin,Dou, Fei,Gao, Lanchang,Hao, Chao,Jin, Jian,Liu, Bi-Feng,Liu, Xin,Xiong, Jiaying,Zhang, Guisen,Zhang, Kunxiao,Zhang, Yifang
, (2020/09/02)
In this study, a series of novel Isoquinolinone derivatives were synthesized as potential multi-target antipsychotics. Among these, compound 13 showed high affinity for dopamine D2 and serotonin 5-HT1A, 5-HT2A, 5-HT6, and 5-HT7 receptors, showed low affinity for off-target receptors (5-HT2C, H1, and α1), and negligible effects on ether-a-gogo-related gene (hERG; i.e., reduced QT interval prolongation). An animal behavioral study revealed that compound 13 reversed APO-induced hyperlocomotion, MK-801-induced hyperactivity, and DOI-induced head twitch. Moreover, compound 13 exhibited a high threshold for acute toxicity, a lack of tendency to induce catalepsy, and did not cause prolactin secretion or weight gain when compared to risperidone. Furthermore, in the forced swim test, tail suspension test, and novel object recognition test, treatment with compound 13 resulted in improvements in depression and cognitive impairment. In addition, compound 13 had a favorable pharmacokinetic profile in rats. Thus, the antipsychotic drug-like effects of compound 13 indicate that it may be useful for developing a novel class of drugs for the treatment of schizophrenia.
LACTAM COMPOUND DERIVATIVE AND APPLICATION THEREOF
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, (2018/10/15)
The present invention relates to a lactam compound derivative, a medicine composition comprising the lactam compound derivative, and uses of the composition and the lactam compound derivative in preparation of a medicine for preventing or treating schizop