title: SYNTHESIS AND STUDY OF HALOGENATED BENZYLAMIDES OF SOME ISOCYCLIC AND HETEROCYCLIC ACIDS AS POTENTIAL ANTICONVULSANTS.
abstract: A series of potential anticonvulsants have been synthesized. There are eight fluorobenzylamides and three chlorobenzylamides of isocyclic or heterocyclic acids. Two not halogenated benzylamides were also synthesized to compare the effect of halogenation. The aim of the research performed was to evaluate whether halogenation of the mother structure is able to improve its anticonvulsant activity. The compounds were tested in Anticonvulsant Screening Project (ASP) of Antiepileptic Drug Development Program (ADDP) of NIH. Compound 1 showed MES ED50 = 80.32 mg/kg, PI = 3.16. Compound 7 showed CKM ED50 = 56.72 mg/kg. Compound 8 showed MES ED50 = 34.23 mg/kg and scPTZ ED50 > 300 mg/kg, PI = 8.53.Compound 13 showed 6Hz ED50 = 78.96, PI = 3.37. The results indicate that fluorination does not improve activity, whereas chlorination in our experiment even reduces it.
authors.forename: Marzanna
authors.initials: M
authors.lastname: Strupińska
authors.forename: Grażyna
authors.initials: G
authors.lastname: Rostafińska-Suchar
authors.forename: Elżbieta
authors.initials: E
authors.lastname: Pirianowicz-Chaber
authors.forename: Mateusz
authors.initials: M
authors.lastname: Grabczuk
authors.forename: Magdalena
authors.initials: M
authors.lastname: Józwenko
authors.forename: Hubert
authors.initials: H
authors.lastname: Kowalczyk
authors.forename: Joanna
authors.initials: J
authors.lastname: Szuba
authors.forename: Monika
authors.initials: M
authors.lastname: Wójcicka
authors.forename: Tracy
authors.initials: T
authors.lastname: Chen
authors.forename: Aleksander P
authors.initials: AP
authors.lastname: Mazurek
mesh_terms: D000147:Acids, Heterocyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D001593:Benzyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D013329:Structure-Activity Relationship
chemical_list: D000147:Acids, Heterocyclic; D000577:Amides; D000927:Anticonvulsants; D001593:Benzyl Compounds