The Fox Chase Chemical Diversity Center, Inc. (FCCDC) in Doylestown PA is a company focused on providing medicinal chemistry/chemical biology support to advance basic research programs. The progress of two such research programs is discussed here.1) Severe seizure activity is associated with recurring cycles of excitotoxicity and oxidative stress that result in progressive neuronal damage and death. Neuroprotection from seizure-related neural damage may be a key strategy for disease modification. Highly potent anticonvulsant agents have been discovered that can completely protect hippocampal neurons from excitotoxicity and oxidative stress.2) Botulinum neurotoxin (BoNT) is the etiological agent that causes the neuroparalytic disease botulism. Inhibition of BoNT serotype A light chain metalloprotease may be important in reversing neuroparalysis as a result of BoNT intoxication. Here, we discuss a class of novel hydroxamic acids which are significantly more potent than reported small molecule inhibitors of the BoNT/A light chain and have improved ADME properties.

Small-molecule anticonvulsant agents with potent in vitro neuroprotection: Enhancing the pharmacokinetic properties of botulinum neurotoxin serotype A protease inhibitors through rational design

244th National Meeting (2012)

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