New derivatives of picolinic acid and nicotinic acid with anticonvulsant activity.
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.
Paruszewski
Ryszard
R
Department of Drug Chemistry, Medical University, 02-097 Warszawa, Poland. rpbw@farm.amwaw.edu.pl
Strupińska
Marzanna
M
Rostafińska-Suchar
Grazyna
G
Stables
James P
JP
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003201:Computers; D015195:Drug Design; D004558:Electric Stimulation; D051379:Mice; D010848:Picolinic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control*; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D010848:Picolinic Acids; C030614:picolinic acid