Bacillus anthracis carries a special type of bacterial toxin and is considered to be a potential biological weapon. The highly lethal spores of B. anthracis cause severe diseases such as cutaneous, gastrointestinal, and inhalation anthrax. The multicomponent binarytoxin (AB-type) of B. anthracis consists of two separate components: component A with enzymatic activity (edema factor and lethal factor) and component B (protective antigen, PA - the binding portion). Component B is essential for the formation of transmembrane channels (PApores) that translocate component A from endosomes to the cytoplasm, thereby causing lethal effects in the target cells. We have designed and synthesized small molecule inhibitors belonging to a novel class of aminoquinolinium substances that block the entry of the enzymatic components through the PA pore.