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杂环基框架作为 5-HT1A 受体激动剂的潜在支架的发展及未来展望：综述。

Development of heterocyclic-based frameworks as potential scaffold of 5-HT1A receptor agonist and future perspectives: A review.

机构信息

School of Acupuncture-Moxibustion and Tuina, Anhui University of Chinese Medicine, Hefei, China.

Gumei Community Health Service Centre, Shanghai Medical College of Fudan University, Shanghai, China.

出版信息

Medicine (Baltimore). 2024 Jun 14;103(24):e38496. doi: 10.1097/MD.0000000000038496.

DOI:10.1097/MD.0000000000038496
PMID:38875413
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11175882/
Abstract

As a subtype of the 5-hydroxytryptamine (5-HT) receptor, 5-HT1A receptors are involved in the pathological process of psychiatric disorders and is an important target for antidepressants. The research groups focus on these area have tried to design novel compounds to alleviate depression by targeting 5-HT1A receptor. The heterocyclic structures is an important scaffold to enhance the antidepressant activity of ligands, including piperazine, piperidine, benzothiazole, and pyrrolidone. The current review highlights the function and significance of nitrogen-based heterocyclics 5-HT1AR represented by piperazine, piperidine, benzothiazole, and pyrrolidone in the development of antidepressant.

摘要

作为 5-羟色胺（5-HT）受体的亚型之一，5-HT1A 受体参与精神疾病的病理过程，是抗抑郁药的重要靶点。关注这些领域的研究小组试图通过靶向 5-HT1A 受体设计新型化合物来缓解抑郁。杂环结构是增强配体抗抑郁活性的重要支架，包括哌嗪、哌啶、苯并噻唑和吡咯烷酮。本综述强调了以哌嗪、哌啶、苯并噻唑和吡咯烷酮为代表的基于氮的杂环 5-HT1AR 在抗抑郁药开发中的作用和意义。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/e90cd502b59e/medi-103-e38496-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/7d9cd56a6c28/medi-103-e38496-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/92db2191dcac/medi-103-e38496-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/b8eb1d99c064/medi-103-e38496-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/a1ead0d8ed5e/medi-103-e38496-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/8bf00aae8fee/medi-103-e38496-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/3100fd3ea063/medi-103-e38496-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/e90cd502b59e/medi-103-e38496-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/7d9cd56a6c28/medi-103-e38496-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/92db2191dcac/medi-103-e38496-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/b8eb1d99c064/medi-103-e38496-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/a1ead0d8ed5e/medi-103-e38496-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/8bf00aae8fee/medi-103-e38496-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/3100fd3ea063/medi-103-e38496-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a1c/11175882/e90cd502b59e/medi-103-e38496-g007.jpg

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Curr Top Med Chem. 2024;24(5):401-415. doi: 10.2174/0115680266280249240126052505.
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Computer-Aided Drug Design and Drug Discovery: A Prospective Analysis.计算机辅助药物设计与药物发现：前瞻性分析
Pharmaceuticals (Basel). 2023 Dec 22;17(1):22. doi: 10.3390/ph17010022.
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Epigenetic regulation in major depression and other stress-related disorders: molecular mechanisms, clinical relevance and therapeutic potential.
表观遗传学在重度抑郁症和其他与应激相关的障碍中的调节：分子机制、临床相关性和治疗潜力。
Signal Transduct Target Ther. 2023 Aug 30;8(1):309. doi: 10.1038/s41392-023-01519-z.
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The Serotonin 1A (5-HT) Receptor as a Pharmacological Target in Depression.5-羟色胺 1A（5-HT）受体在抑郁症中的药理学靶点作用。
CNS Drugs. 2023 Jul;37(7):571-585. doi: 10.1007/s40263-023-01014-7. Epub 2023 Jun 29.
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Editorial: Six-membered heterocycles: their synthesis and bio applications.社论：六元杂环：其合成及生物应用
Front Chem. 2023 Jun 8;11:1229825. doi: 10.3389/fchem.2023.1229825. eCollection 2023.
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