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The Design and Synthesis of a Series of ß-Heteroaryl-ß-Amino Acids as Putative Anti-Epileptogenic Agents Disclosure Number: IPCOM000004830D
Publication Date: 2001-Jun-26

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Patent/Patent Application:
09/041,371 [+details]


Epilepsy is a neurologic disorder characterized by spontaneous recurrent seizures arising from abnormal electrical activity in the brain. Commercially available drugs for the treatment of epilepsy are merely symptomatic, diminishing the frequency of seizures rather than affecting the biochemical basis of the disorder. Effective seizure control is achieved for only 60-70 % of those receiving treatment, with 40-45 % of those treated developing side effects ranging from cosmetic to life threatening. Clearly, a need exists for new therapeutic agents with improved efficacy and tolerability. Our research is focused on the design and synthesis of putative small molecule drugs, which simultaneously block the glycine co-agonist site on the excitatory N-methyl-D-aspartate (NMDA) receptor while reducing glial uptake of the inhibitory neurotransmitter ß-aminobutyric acid (GABA). This poster highlights the design and synthesis of a series of ß-heteroaryl-ß-amino acids. These compound were prepared in four facile steps starting from the corresponding ß-heteroarylaldehydes. In vivo evaluation of these molecules will also be presented.