Synthesis of novel 3-(alkylcarbamoyl)-2-aryl-1,2-dihydro-6,7-(methylenedioxy)-3H-quinazolin-4-ones as anticonvulsant agents.
A series of 3-(alkylcarbamoyl)-2-aryl-1,2-dihydro-6,7-(methylenedioxy)-3H-quinazolin-4-ones, compounds 3-6, were synthesized, and screened as anticonvulsant agents in DBA/2 mice against sound-induced seizure (Table). The new compounds were found to display anticonvulsant properties inferior to those of the known dehydro congeners 1 and 2. The binding affinities of 1-6 at the AMPA and NMDA receptors were also evaluated.
Micale
Nicola
N
Dipartimento Farmaco-Chimico, Università degli Studi di Messina, Viale Annunziata, I-98168 Messina. nmicale@pharma.unime.it
Postorino
Giovanna
G
Grasso
Silvana
S
Zappalà
Maria
M
Zuccalà
Giuseppe
G
Ferreri
Guido
G
De Sarro
Giovambattista
G
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D015507:Drugs, Investigational / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D051379:Mice; D008811:Mice, Inbred DBA; D011485:Protein Binding / Q000502:physiology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D051381:Rats; D012640:Seizures / Q000517:prevention & control
D000927:Anticonvulsants; D015507:Drugs, Investigational; D011799:Quinazolines