Synthesis and Anticonvulsant Activity of Substituted-1,3-diazaspiro[4.5]decan-4-ones

Autor:	Mohamed Nabil, Aboul-Enein, Aida Abdel Sattar, El-Azzouny, Ola Ahmed, Saleh, Kamilia Mahmoud, Amin, Yousreya Ali, Maklad, Rasha Mohamed, Hassan
Rok vydání:	2015
Předmět:	Male Electroshock Behavior Animal Molecular Structure Imidazoles Brain Motor Activity Disease Models Animal Mice Structure-Activity Relationship Seizures Drug Design Animals Pentylenetetrazole Anticonvulsants
Zdroj:	Archiv der Pharmazie. 348(8)
ISSN:	1521-4184
Popis:	A series of novel spiroimidazolidinone derivatives 6a-d and 8a-x were synthesized and biologically evaluated for their anticonvulsant activity in the maximal electroshock seizure (MES) assay and the subcutaneous pentylenetetrazole (scPTZ) screening test. Compound 8w was the most active derivative in the scPTZ screening test with an ED50 value by about 5- and 83.6-fold lower than those of phenobarbital and ethosuximide as reference drugs, respectively. Most of the tested compounds exhibited moderate to weak activity in the MES screen test, except for 8a which displayed 100% protection at 0.09 mmol/kg. Moreover, all the test compounds did not show any minimal motor impairment in the neurotoxicity test.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::dee4e6eb471707bdb9f0f65e88571d30 https://pubmed.ncbi.nlm.nih.gov/26032619 Zobrazit plný text záznamu Plný text