Citation: 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. doi: 10.1016/j.cclet.2006.11.022 shu

Pharmacophore-guided design, synthesis and evaluation of quinazoline-arylpiperazines as new α₁-adrenoceptor antagonists

Hao Fang ^a, ,
Min Yong Li ^b ,
Lin Xia ^b

a School of Pharmacy, Shandong University, Jinan 250012, China;
b Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China

Received Date: 16 May 2006

Fund Project: 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).

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.
- α₁-Adrenoceptor,
- Antagonists,
- Pharmacophore-guided design
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