• Bioorg. Med. Chem. Lett. · Jul 2008

    Design, synthesis, and evaluation of bisubstrate analog inhibitors of cholera toxin.

    • Guangtao Zhang.
    • Department of Chemistry, University of Washington, PO Box 351700, Seattle, WA 98195, USA. windzgt@gmail.com
    • Bioorg. Med. Chem. Lett. 2008 Jul 1; 18 (13): 3724-7.

    AbstractBisubstrate analog inhibitors in which a nicotinamide mimic is attached to a series of structurally diversified guanidines (arginine mimics) were synthesized and evaluated for inhibition of cholera toxin. The mechanism-based bisubstrate inhibitors were up to 1400-fold more potent than the natural substrate NAD+ and 400-fold more potent than the artificial substrate diethylamino (benzylidine-amino)guanidine (DEABAG) in an assay toward an intrinsically active mutant of wild-type cholera toxin.

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