Bioactivity-guided synthesis of gramine derivatives as new MT1 and 5-HT1A receptors agonists
文献类型：期刊论文
| 作者 | Yin, Xiu-Juan1,2,4; Huang, Xiao-Yan2,3; Ma, Yun-Bao2,3; Geng, Chang-An2,3 ; Li, Tian-Ze2,3; Chen, Xing-Long2,4; Yang, Tong-Hua2,3; Zhou, Jun1,2; Zhang, Xue-Mei2,3; Chen, Ji-Jun2,3
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| 刊名 | JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
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| 出版日期 | 2017 |
| 卷号 | 19期号:6页码:610-622 |
| 关键词 | Gramine melatonin receptor 5-hydroxy-tryptamine receptor agonistic activity structure-activity relationships |
| 英文摘要 | Twenty-four gramine derivatives were synthesized and evaluated on MT1 and 5-HT1A receptors in vitro. Among them, seven derivatives (7, 8, 16, 19, 20, 21, and 24) exhibited higher agonisting activities on MT1 or 5-HT1A receptors. Compared with gramine, derivatives 7, 8, 16, 19, 20, 21, and 24 displayed 1.6-3.5-fold increase in agonistic rates on 5-HT1A receptor. Particularly, derivatives 7, 19, and 21 exhibited significant agonistic activities on MT1 and 5-HT1A receptors with EC50 values of 0.51, 0.39, 0.50 m. and 0.28, 0.46, 0.23 m., respectively. The preliminary structure-activity relationships of gramine derivatives were summarized for further investigation on MT1 and 5-HT1A receptors as new potential agonists. |
| 类目[WOS] | Plant Sciences ; Chemistry, Applied ; Chemistry, Medicinal ; Pharmacology & Pharmacy |
| 研究领域[WOS] | Plant Sciences ; Chemistry ; Pharmacology & Pharmacy |
| 关键词[WOS] | MELATONIN RECEPTORS ; PINEAL-GLAND ; IDENTIFICATION ; ANTAGONISTS ; SUBTYPES |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000401984100010 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/51247]  |
| 专题 | 昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室 |
| 作者单位 | 1.Yunnan Univ, Sch Chem Sci & Technol, Kunming 650091, Peoples R China 2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China 3.Chinese Acad Sci, Kunming Inst Bot, Yunnan Key Lab Nat Med Chem, Kunming 650201, Peoples R China 4.Univ Chinese Acad Sci, Kunming Inst Bot, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yin, Xiu-Juan,Huang, Xiao-Yan,Ma, Yun-Bao,et al. Bioactivity-guided synthesis of gramine derivatives as new MT1 and 5-HT1A receptors agonists[J]. JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH,2017,19(6):610-622. |
| APA | Yin, Xiu-Juan.,Huang, Xiao-Yan.,Ma, Yun-Bao.,Geng, Chang-An.,Li, Tian-Ze.,...&Chen, Ji-Jun.(2017).Bioactivity-guided synthesis of gramine derivatives as new MT1 and 5-HT1A receptors agonists.JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH,19(6),610-622. |
| MLA | Yin, Xiu-Juan,et al."Bioactivity-guided synthesis of gramine derivatives as new MT1 and 5-HT1A receptors agonists".JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH 19.6(2017):610-622. |
入库方式： OAI收割
来源：昆明植物研究所
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