ChemInform Abstract: Synthesis of a New Homologous Series of p-Chlorophenyl Alcohol Amides, Their Anticonvulsant Activity and Their Testing as Potential GABAB Receptor Antagonists

Autor:	Meza-Toledo Se, E. Juarez‐Carvajal, Carvajal-Sandoval G
Rok vydání:	2010
Předmět:	Stereochemistry organic chemicals medicine.medical_treatment Alcohol General Medicine GABAB receptor Para position Homologous series chemistry.chemical_compound Anticonvulsant chemistry Peak effect medicine Potency Pentylenetetrazol medicine.drug
Zdroj:	ChemInform. 29
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.199851289
Popis:	The anticonvulsant activity of a homologous series of p-chlorophenyl alcohol amides is described. The new compounds (+/-)-2-hydroxy-2-(4'-chlorophenyl)-butyramide (2), (+/-)-3- hydroxy-3-(4'-chlorophenyl)pentanamide (4) and (+/-)-4-hydroxy-4-(4'-chlorophenyl)-hexanamide (6), were prepared and tested for their anticonvulsant activity. Compounds 2, 4, and 6 exhibited significant activity in seizures provoked by pentylenetetrazol. Chlorine in the para position of the phenyl ring increased both their potency at the peak effect and the duration of their anticonvulsant activity. The anticonvulsant activities of (+/-)-3-hydroxy-3-phenylpentanamide (3) and compound 4 were antagonized by DL-baclofen. This, and the protecting activity of 3 in the genetic-absence-epilepsy rats of the Strasbourg model suggest that the phenyl alcohol amides could be GABAB receptor antagonists.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::500d6d1b7081f94180e138e834933846 https://doi.org/10.1002/chin.199851289 Zobrazit plný text záznamu Plný text