Synthesis and phosphodiesterase type-5 inhibitory activity of sildenafil analogues possessing a guanidine group in the phenyl ring
文献类型：期刊论文
| 作者 | Shi J(石静); Liu Z(刘正); Wang Z(王 震); Tian GH(田广辉); Yang XJ(杨小军); Wang XL(王雪兰); Sun HB(孙宏斌); Shen JS(沈敬山)
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| 刊名 | Journal of China Pharmaceutical University
 |
| 出版日期 | 2010 |
| 卷号 | 41期号:2页码:112-117 |
| 关键词 | sildenafil analogues guanidine group PDE5 inhibitor |
| ISSN号 | 1000-5048 |
| 其他题名 | 苯环上含有胍基的西地那非类似物的合成及磷酸二酯酶5抑制活性(英文) |
| 文献子类 | Article |
| 英文摘要 | In this study,a series of new sildenafil analogues 11-27 possessing a guanidine group were synthesized to investigate their PDE5 inhibitory activity and selectivity using [3H] cGMP SPA kit in vitro and efficacy in the rat model of erection. Most of the compounds showed potent activity against PDE5, and more importantly, several compounds exhibited higher PDE5 selectivity over PDE6 than that of sildenafil. Structure-activity relationship of these sildenafil analogues was also discussed. Within this series of compounds, compound 15(IC50=1.7 nmol/L) not only exhibited more potent PDE5 inhibitory activity than that of sildenafil (IC50=6.5 nmol/L), but also showed functional efficacy in the rat model of erection |
| 资助项目 | National High Technology Research and Development Program of China"863 Prograsm"[00000000] ; China National Key Hi-Tech Innovation Project for the R&D of Novel Drugs[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3993035 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/267941]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. 2.Center for Drug Discovery, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.; 3.Topharman Shanghai Co., Ltd., Shanghai 201209, China.; |
| 推荐引用方式 GB/T 7714 | Shi J,Liu Z,Wang Z,et al. Synthesis and phosphodiesterase type-5 inhibitory activity of sildenafil analogues possessing a guanidine group in the phenyl ring[J]. Journal of China Pharmaceutical University,2010,41(2):112-117. |
| APA | 石静.,刘正.,王 震.,田广辉.,杨小军.,...&沈敬山.(2010).Synthesis and phosphodiesterase type-5 inhibitory activity of sildenafil analogues possessing a guanidine group in the phenyl ring.Journal of China Pharmaceutical University,41(2),112-117. |
| MLA | 石静,et al."Synthesis and phosphodiesterase type-5 inhibitory activity of sildenafil analogues possessing a guanidine group in the phenyl ring".Journal of China Pharmaceutical University 41.2(2010):112-117. |
入库方式： OAI收割
来源：上海药物研究所
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