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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.