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 Lin Xia Bin Wu Tao Wang Zhen Zhou Jiang

引用本文: 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
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

  • 基金项目:

    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.

摘要: 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.

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  • 收稿日期:  2008-04-15
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