The invention provides low molecular weight compounds that block the pore
formed by protective antigen and inhibit anthrax toxin action. Structures
of the compounds are derivatives of .beta.-cyclodextrin. Per-substituted
alkylamino derivates displayed inhibitory activity, and they were
protective against anthrax lethal toxin action at low micromolar
concentrations. Also, the addition of one of the alkylamino derivatives
to the bilayer lipid membrane with multiple PA channels caused a
significant decrease in membrane conductance. Thus, the invention also
provides methods for protection against anthrax toxicity.