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Synthesis and Anticonvulsant Activity of Acetylenic Quinazolinone Derivatives
Author(s) -
Usifoh Cyril O.,
Scriba Gerhard K. E.
Publication year - 2000
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 - 10.1002/1521-4184(20008)333:8<261::aid-ardp261>3.0.co;2-o
Subject(s) - anticonvulsant , chemistry , carbamazepine , phenytoin , ed50 , quinazolinone , neurotoxicity , pharmacology , seizure threshold , stereochemistry , epilepsy , toxicity , medicine , biochemistry , organic chemistry , receptor , psychiatry
Acetylenic derivatives of quinazolinones and quinazolinediones were synthesized and evaluated for their anticonvulsant activity. Most compounds displayed seizure‐antagonizing activity in the maximal electroshock test (MES test) in most cases associated with little or no acute neurotoxicity determined in the rotorod test. Only three compounds exhibited significant activity in the seizure threshold test with subcutaneous pentylenetetrazole (scMet test). Based on the ED 50 in the MES test, 1,3‐bis‐(prop‐2‐ynyl)‐quinazoline‐2,4‐(1 H ,3 H )‐dione ( 9a ) was about ten‐fold less active than phenytoin or carbamazepine but about as active as mesuximide.