The Clostridium botulinum bacterium is commonly found in soil and produces a neurotoxin which paralyzes muscles, leading to difficulty swallowing, talking, and breathing. Due to the availability and potency of this neurotoxin, its potential use as a bioweapon poses a threat to the human population. Botulinum toxin A is also the main component of BOTOX, an injectable drug used to calm muscle spasms and cosmetically remove facial wrinkles. An inhibitor of the botulinum toxin is needed in case people are exposed to elevated concentrations of the toxin. Our project involves synthesizing analogs of a previously identified potential inhibitor. We systematically varied several components of the synthesis to determine the effect that the changes would have on the compound's inhibitory ability. We also initiated the synthesis of a 4-substituted-quinoline, a component of these reactions with a unique substitution pattern. We will present the results of our syntheses and HPLC bioassays.

Inhibitors of botulinum neurotoxin A: Synthesis and biological activity

245th National Meeting (2013)

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