Abstract: As the infection of the acquired immunodeficiency syndrome (AIDS) and the mutation of the HIV virus keep increasing,there’s an urgent demand for developing new anti-HIV drugs.Up till now,the research on anti-HIV agents has been carried out in two ways:based on known targets or new targets.Ribonuclease H (RNase H),which has with its own unique catalytic sites of enzyme function and is regarded as a novel drug target for anti-HIV therapy,is a domain of the reverse transcriptase.This review summarizes RNase H inhibitors discovered in recent years and explains their mechanisms of action which aims at providing some useful information for further structural modifications and design of RNase H inhibitors.