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New Derivatives of Picolinic Acid and Nicotinic Acid with Anticonvulsant Activity

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Abstract:

Previously obtained Pic-BZA is a potent anticonvulsant with low neurotoxicity, but its half-time of action is only about 15 min. In search for equally effective anticonvulsants but with a longer time of action fourteen Pic-BZA analogs were obtained. The compounds were evaluated in the Anticonvulsant Screening Project (ASP) of Antiepileptic Drug Development Program (ADDP) of NIH. Picolinic acid 2-fluorobenzylamide (Pic-2-F-BZA, 7) appeared to be the most effective compound of the series.

Keywords: activity; anticonvulsant; neurotoxicity; nicotinic acid; picolinic acid; time of action

Document Type: Review Article

DOI: https://doi.org/10.2174/0929866054696046

Affiliations: Department of Drug Chemistry, Medical University, 02-097 Warszawa, Poland;

Publication date: 2005-10-01

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  • Protein & Peptide Letters publishes short papers in all important aspects of protein and peptide research, including structural studies, recombinant expression, function, synthesis, enzymology, immunology, molecular modeling, drug design etc. Manuscripts must have a significant element of novelty, timeliness and urgency that merit rapid publication. Reports of crystallisation, and preliminary structure determinations of biologically important proteins are acceptable. Purely theoretical papers are also acceptable provided they provide new insight into the principles of protein/peptide structure and function.
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