A series of nitric oxide-donating derivatives of [1,2,4]triazol-5(4H)-one (9a-f and 15a-f) as a novel class of angiotensin Ⅱ receptor ATl antagonists have been designed and synthesized by coupling furoxan and nitric oxide with lead compound 1.The synthesized compounds were evaluated for their antagonism of ATl receptor with induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9b, 15b and 15e exhibited potent antagonistic activity of ATl receptor.Moreover 9b, 15d, 15e, had good maximum NO release amount of this series.