| Pharmacophore-guided design, synthesis and evaluation of quinazoline-arylpiperazines as new α1-adrenoceptor antagonists |
| |
| 作者姓名： | Hao Fang Min Yong Li Lin Xia |
| |
| 作者单位： | a，* |
| |
| 基金项目： | We gratefully acknowledge Dr. Ting Wang （European Molecular Biology Laboratory, Germany） for the use of 3DFS program. This work was supported by the National High-Tech Research and Development Plan （No. 2002AA2Z3118）. |
| |
| 摘 要： | A series of arylpiperazinesquinazoline-2,4-diamine compounds were designed and synthesized based on pharmacophore for uro-selectiveα_1-adrenoceptor antagonists and 3D chemical database searching.The in vitro functional analysis showed that compounds 9 and 14 showed better and similarα_1-AR antagonistic activity compared with prazosin.
|
| 关 键 词： | α_1-Adrenoceptor Antagonists Pharmacophore-guided design |
| 收稿时间： | 2006-05-16 |
Pharmacophore-guided design,synthesis and evaluation of quinazoline-arylpiperazines as new α1-adrenoceptor antagonists |
| |
| Hao Fang Min Yong Li Lin Xia.Pharmacophore-guided design,synthesis and evaluation of quinazoline-arylpiperazines as new α1-adrenoceptor antagonists[J].Chinese Chemical Letters,2007,18(1):41-44. |
| |
| Authors: | Hao Fang Min Yong Li Lin Xia |
| |
| Institution: | 1. School of Pharmacy, Shandong University, Jinan 250012, China;2. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China |
| |
| Abstract: | A series of arylpiperazinesquinazoline-2,4-diamine compounds were designed and synthesized based on pharmacophore for uro-selective α1-adrenoceptor antagonists and 3D chemical database searching. The in vitro functional analysis showed that compounds 9 and 14 showed better and similar α1-AR antagonistic activity compared with prazosin. |
| |
| Keywords: | |
| 本文献已被 CNKI 维普 ScienceDirect 等数据库收录！ |
