Synthesis and anticonvulsant properties of 2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-ones.
A series of 2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-ones were synthesized and evaluated for anticonvulsant activity in DBA/2 mice against sound-induced seizures and in rats against maximal electroshock-induced seizures. Most of the derivatives showed an anticonvulsant effect better than that of valproate, a commonly used anticonvulsant drug. Compound 3 possessed an anticonvulsant activity comparable to that of diphenylhydantoin in both tests and was selected for further studies. Structure-activity relationships are discussed.
Chimirri
A
A
Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Annunziata, Italy.
De Sarro
A
A
De Sarro
G
G
Grasso
S
S
Trimarchi
G R
GR
Zappalà
M
M
D000161:Acoustic Stimulation; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000627:therapeutic use; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D004353:Drug Evaluation, Preclinical; D004597:Electroshock; D005260:Female; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D011760:Pyrrolidinones / Q000138:chemical synthesis* / Q000627:therapeutic use; D051381:Rats; D011919:Rats, Inbred Strains; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D001562:Benzimidazoles; D011760:Pyrrolidinones