Anthrax is a malignant infectious disease caused by Bacillus anthracis spores,after entering the host Bacillus an-thracis produces and releases anthrax toxin,which is the main cause leading to death of the host. The anthrax toxin is composed of two enzymatically active components:lethal factor(LF)and edema factor(EF),and one shared receptor binding and translocation com-ponent:protective antigen(PA). PA combined with LF is called lethal toxin(LeTx),while PA combined with EF called edema toxin (EdTx). Currently,the main drugs for treating anthrax are antibiotics,but antibiotics can only kill part of anthrax spores and bacte-ria,and cannot inhibit the activity of anthrax toxin. So it is necessary to develop novel drugs for inhibiting anthrax toxin. This review summarizes the evolution of small-molecule inhibitors of anthrax toxin respectively targeting PA,LF and EF.