title: New derivatives of picolinic acid and nicotinic acid with anticonvulsant activity.
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.
authors.affiliation: Department of Drug Chemistry, Medical University, 02-097 Warszawa, Poland. rpbw@farm.amwaw.edu.pl
authors.forename: Ryszard
authors.initials: R
authors.lastname: Paruszewski
authors.forename: Marzanna
authors.initials: M
authors.lastname: Strupińska
authors.forename: Grazyna
authors.initials: G
authors.lastname: Rostafińska-Suchar
authors.forename: James P
authors.initials: JP
authors.lastname: Stables
mesh_terms: 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
chemical_list: D000927:Anticonvulsants; D010848:Picolinic Acids; C030614:picolinic acid