In　the　present　study,　a　series　of　3-benzylquinazolin-4(3H)-ones　were　synthesized　and　characterized.　Their　vasodilative　effects　were　evaluated　by　wire　myograph　on　isolated　rat　mesenteric　arterial　ring　induced　contraction　with　60　mM　KCl.　The　SAR　of　target　compounds　was　discussed　preliminarily.　Among　these　compounds,　2a　and　2c　displayed　potent　vasodilatation　action　and　could　compete　significantly　the　rat　mesenteric　arterial　rings　induced　contraction　with　phenylephrine.　Compounds　2a　and　2c　were　further　tested　for　their　antihypertensive　effects　in　SHR　by　oral　administration.　The　results　indicated　that　2a　and　2c　could　reduce　significantly　both　diastolic　and　systolic　blood　pressure.　Moreover,　2c　displayed　antihypertensive　effect　in　a　dose　dependent　manner,　and　could　maintain　the　effects　for　6　h　at　a　dosage　of　4.0　mg/kg.　These　findings　suggest　that　the　title　compounds　are　novel　vasodilative　agents,　representing　a　novel　series　of　promising　antihypertensive　agents.　(C)　2014　Elsevier　Ltd.　All　rights　reserved.