ORGN 162 |
| Based on the HTS hit NSC 357756, we have developed a new series of inhibitors of BoNTs. Botulinum neurotoxins (BoNTs), produced by bacteria Clostridium botulinum in contaminated food, are the deadliest toxins known. Among the seven BoNT serotypes (A-G), BoNT A has been used for the treatment of muscle hyperactivity and spasticity disorders, as well as cosmetic applications, raising the concern of overdosing. Furthermore, BoNTs have been recognized as a potential biological weapon. Based on the reported inhibitory activities of NSC 240898 and NSC 377363, we synthesized two series of benzimidazole and indole analogs. A key aspect of our synthesis was the use of microwave heating for SNAr reactions, Sonogashira couplings, and Au(I)-catalyzed indole formations. |
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Total Synthesis, Materials, Devices and Switches, Molecular Recognition and Self-Assembly, Biologically-Related Molecules and Processes
8:00 PM-10:00 PM, Sunday, August 19, 2007 BCEC -- Exhibit Hall - B2, Poster
Division of Organic Chemistry |