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Synthesis and Anticonvulsant Activity of Substituted‐1,3‐diazaspiro[4.5]decan‐4‐ones
Author(s) -
AboulEnein Mohamed Nabil,
ElAzzouny Aida Abdel Sattar,
Saleh Ola Ahmed,
Amin Kamilia Mahmoud,
Maklad Yousreya Ali,
Hassan Rasha Mohamed
Publication year - 2015
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201500092
Subject(s) - ethosuximide , anticonvulsant , ed50 , chemistry , neurotoxicity , phenobarbital , pharmacology , active compound , stereochemistry , toxicity , epilepsy , medicine , biochemistry , organic chemistry , in vitro , psychiatry
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 ED 50 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.