Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors
文献类型：期刊论文
| 作者 | Luo, Na1; Fang, Xiaoyu1; Su, Mingbo2; Zhang, Xinwen2; Li, Dan3; Li, Honglin1; Li, Shiliang1; Zhao, Zhenjiang1 |
| 刊名 | CHINESE JOURNAL OF CHEMISTRY
 |
| 出版日期 | 2021-09-01 |
| 卷号 | 39期号:1页码:115-120 |
| 关键词 | Type II diabetes Dipeptidyl peptidase IV Inhibitors Molecular docking Structure‐ activity relationship |
| ISSN号 | 1001-604X |
| DOI | 10.1002/cjoc.202000342 |
| 文献子类 | Article |
| 英文摘要 | Main observation and conclusion Dipeptidyl peptidase 4 (DPP-4) is a clinically validated target for the treatment of type 2 diabetes mellitus (T2DM). To discover novel and potent DPP-4 inhibitors, three series of compounds were designed and synthesized in this study based on our previously identified novel scaffold of 2-phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine. Among the designed compounds, 41d-1 was the most potent one with an IC50 value of 16.00 nM. Besides, 41d-1 (5 mg/kg) displayed a moderate glucose tolerance capability in ICR mice. Structure-activity-relationship (SAR) studies were discussed in detail, which is constructive for our further optimization. |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000601113600016 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309402]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Li, Shiliang; Zhao, Zhenjiang |
| 作者单位 | 1.East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zhuchongzhi Rd, Shanghai 201203, Peoples R China; 3.Shandong Biopolar Dichang Pharmaceut Co Ltd, RM2306,786 Linzi Ave, Zibo 255400, Shandong, Peoples R China |
| 推荐引用方式 GB/T 7714 | Luo, Na,Fang, Xiaoyu,Su, Mingbo,et al. Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors[J]. CHINESE JOURNAL OF CHEMISTRY,2021,39(1):115-120. |
| APA | Luo, Na.,Fang, Xiaoyu.,Su, Mingbo.,Zhang, Xinwen.,Li, Dan.,...&Zhao, Zhenjiang.(2021).Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors.CHINESE JOURNAL OF CHEMISTRY,39(1),115-120. |
| MLA | Luo, Na,et al."Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors".CHINESE JOURNAL OF CHEMISTRY 39.1(2021):115-120. |
入库方式： OAI收割
来源：上海药物研究所
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