Citation: Jia Bin Li, Lin Xia, Bin Wu, Tao Wang, Zhen Zhou Jiang. Design, synthesis and biological estimation of 1-(benzoxazole-2-y1)piperazine and 4-(benzoxazole-2-yl)piperidine derivatives as potential α₁-AR antagonists[J]. Chinese Chemical Letters, ;2008, 19(10): 1193-1195. doi: 10.1016/j.cclet.2008.06.042 shu

Design, synthesis and biological estimation of 1-(benzoxazole-2-y1)piperazine and 4-(benzoxazole-2-yl)piperidine derivatives as potential α₁-AR antagonists

Jia Bin Li ^a, ,
Lin Xia ^b ,
Bin Wu ^d ,
Tao Wang ^c ,
Zhen Zhou Jiang ^c

a Department of Inorganic Chemistry, China Pharmaceutical University, Nanjing 210009, China;
b Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;
c National Drug Screening Center, China Pharmaceutical University, Nanjing 210009, China;
d School of Pharmacy, Nanjing Medical University, Nanjing 210029, China

Received Date: 15 April 2008

Fund Project: This work was supported by the National High-Tech Research and Development Plan (No. 2002AA2Z3118). We also thank Prof. Xiaowen Xue for general help in manuscript preparation.

Two series of 1-(benzoxazole-2-yl) piperazine(8a-i) and 4-(benzoxazole-2-yl) piperidine compounds(10a-i) were designed,synthesized and evaluated for their α₁-AR antagonistic activities.Biological assay in vitro indicated that 10h showed slightly stronger α₁-AR antagonistic activity to that of our lead compound 1.
- BPH,
- α₁-AR antagonists,
- Benzoxazole,
- Piperidine,
- Piperazine
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