Exploration of o-spiroketal c-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (sglt2) inhibitors
文献类型：期刊论文
| 作者 | Lv, Binhua1,2,3; Xu, Baihua1,2,3; Feng, Yan3; Peng, Kun3; Xu, Ge3; Du, Jiyan3; Zhang, Lili3; Zhang, Wenbin3; Zhang, Ting3; Zhu, Liangcheng3 |
| 刊名 | Bioorganic & medicinal chemistry letters
 |
| 出版日期 | 2009-12-15 |
| 卷号 | 19期号:24页码:6877-6881 |
| 关键词 | O-spiroketal c-arylglucosides Sglt2 Spiro[isobenzofuran-1, 2 '-pyran] Glucosuria Blood glucose |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2009.10.088 |
| 通讯作者 | Lv, binhua(51popo51@163.com) |
| 英文摘要 | A series of novel o-spiroketal c-arylglucosides have been prepared and evaluated in cell-based functional assays for activity against human sodium-dependent glucose co-transporters 1 and 2 ( sglt1 and 2). the core spiro[isobenzofuran-1,2'-pyran] structure proved to be an effective scaffold for diversification and a number of compounds with single digit nanomolar potency and high selectivity have been synthesized. compound 5a promoted glucosuria when administered in vivo in rats and produced a significant blood glucose reduction effect. (c) 2009 elsevier ltd. all rights reserved. |
| WOS关键词 | REABSORPTION ; MUTATION ; TYPE-2 ; LEVEL |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| WOS类目 | Chemistry, Medicinal ; Chemistry, Organic |
| 语种 | 英语 |
| WOS记录号 | WOS:000271724200011 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| URI标识 | http://www.irgrid.ac.cn/handle/1471x/2395065 |
| 专题 | 中国科学院大学 |
| 通讯作者 | Lv, Binhua |
| 作者单位 | 1.Chinese Acad Sci, Chengdu Inst Organ Chem, Chengdu 610041, Peoples R China 2.Chinese Acad Sci, Grad Sch, Beijing 100049, Peoples R China 3.Egret Pharma Shanghai Co Ltd, Shanghai 201203, Peoples R China 4.Theracos Inc, Sunnyvale, CA 94805 USA |
| 推荐引用方式 GB/T 7714 | Lv, Binhua,Xu, Baihua,Feng, Yan,et al. Exploration of o-spiroketal c-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (sglt2) inhibitors[J]. Bioorganic & medicinal chemistry letters,2009,19(24):6877-6881. |
| APA | Lv, Binhua.,Xu, Baihua.,Feng, Yan.,Peng, Kun.,Xu, Ge.,...&Chen, Yuanwei.(2009).Exploration of o-spiroketal c-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (sglt2) inhibitors.Bioorganic & medicinal chemistry letters,19(24),6877-6881. |
| MLA | Lv, Binhua,et al."Exploration of o-spiroketal c-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (sglt2) inhibitors".Bioorganic & medicinal chemistry letters 19.24(2009):6877-6881. |
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来源：中国科学院大学
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