Abstract: Adenovirus is a common cause of infection in children and adults with acute respiratory tract, gastrointestinal tract and urinary tract. It can cause serious and even fatal infections in patients with low immune function. Therefore, it poses a great threat to human health. Currently, there are no specific anti-adenoviral drugs in market. With in-depth investigation of the pathogenic mechanism and biological characteristics of adenovirus, and the rapid development of drug screening technology, new generation of anti-adenovirus drug targets and related inhibitors have been discovered, providing new options for treatment. This review selects the representative case studies in recent years and summarizes the advances in anti-adenoviral medicinal chemistry.