title: A new homologous series of anticonvulsants: phenyl alcohol amides. Synthesis and pharmacological evaluation.
abstract: The anticonvulsant activity of a homologous series of phenyl alcohol amides is described. (+-)-2-Hydroxy-2-phenylbutyramide (1), (+-)-3-hydroxy-3-phenylpentanamide (2) and (+-)-4-hydroxy-4-phenylhexanamide (3) were prepared and tested for their anticonvulsant profile and neurotoxicity. 1, 2 and 3 exhibited a broad profile of anticonvulsant activity and a similar significant activity in the seizures provoked by maximal electroshock, pentetrazol, 4-aminopyridine, bicuculline and thiosemicarbazide, but in the strychnine and picrotoxin tests, the protection was variable. The rotarod ataxia test was used to evaluate their neurotoxicity. In this test 2 possesses the lowest neurotoxicity.
authors.affiliation: Departamento de Bioquímica, Escuela Nacional de Ciencias Biológica, Instituto Politécnico Nacional (IPN), Mexico City, Mexico.
authors.forename: S E
authors.initials: SE
authors.lastname: Meza-Toledo
authors.forename: M T
authors.initials: MT
authors.lastname: Zenteno-García
authors.forename: E
authors.initials: E
authors.lastname: Juárez-Carvajal
authors.forename: D
authors.initials: D
authors.lastname: Martínez-Muñoz
authors.forename: G
authors.initials: G
authors.lastname: Carvajal-Sandoval
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004597:Electroshock; D006880:Hydroxy Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D010654:Phenylbutyrates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004856:Postural Balance / Q000187:drug effects; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control
chemical_list: D000577:Amides; D000927:Anticonvulsants; D006880:Hydroxy Acids; D010654:Phenylbutyrates; C068957:3-hydroxy-3-phenylpentamide; C068956:2-hydroxy-2-phenylbutyramide; C020361:gamma-hydroxy-gamma-ethyl-gamma-phenylbutyramide