A pair of triazole-linked bistetrahydrobenzofuran derivatives were prepared in high yields through Cu (II)-catalyzed click reaction under mild conditions. All of the intermediates and target compounds were characterized by NMR, IR, ESI-MS and elemental analysis. Thein vitroH+/K+-ATPase inhibitory effect for the target compounds were also evaluated by MTT methods, and the (E)-isomer of the bistetrahydrobenzofurans exhibited the better H+/K+-ATPase inhibitory activities than the commercial omeprazole with the IC50of 37.90 μM. The bioactive compound might be potentially used as anti-ulcer agents in the treatment of acid-related diseases.