Design, Synthesis, and Biological Evaluation of 8-Phenyl-THIQ as Antidepressive Agents

IF 4.2 4区医学 Q2 CHEMISTRY, MEDICINAL

Drug Development Research Pub Date : 2025-09-08 DOI:10.1002/ddr.70156

Xiaopeng Wei, Fan Yang, Nuo Xu, Xingyu Huang, Wei Qiao

引用次数: 0

Abstract

The structural modification and derivatization of natural products represent an essential pathway for pharmaceutical innovation in the management of depression. The 8-phenyl tetrahydroisoquinoline, as a parent core, was obtained from magnoflorine by a structural simplification strategy. The present report details the synthesis and antidepressant activity studies of 8-phenyl-THIQ analogs. Among them, compounds 1e and 1j exhibited significant antidepressant activity in addition to high synthetic accessibility and adequate predictive ADME/T properties.

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8-苯基thiq抗抑郁药物的设计、合成和生物学评价

天然产物的结构修饰和衍生化是治疗抑郁症药物创新的重要途径。8-苯基四氢异喹啉作为亲本核心，通过结构简化策略从木兰碱中得到。本报告详细介绍了8-苯基thiq类似物的合成和抗抑郁活性研究。其中，化合物1e和1j具有显著的抗抑郁活性，且具有较高的合成可及性和足够的ADME/T预测性能。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Drug Development Research 医学-药学

CiteScore

6.40

自引率

2.60%

发文量

104

审稿时长

6-12 weeks

期刊介绍： Drug Development Research focuses on research topics related to the discovery and development of new therapeutic entities. The journal publishes original research articles on medicinal chemistry, pharmacology, biotechnology and biopharmaceuticals, toxicology, and drug delivery, formulation, and pharmacokinetics. The journal welcomes manuscripts on new compounds and technologies in all areas focused on human therapeutics, as well as global management, health care policy, and regulatory issues involving the drug discovery and development process. In addition to full-length articles, Drug Development Research publishes Brief Reports on important and timely new research findings, as well as in-depth review articles. The journal also features periodic special thematic issues devoted to specific compound classes, new technologies, and broad aspects of drug discovery and development.