Structure-activity relationships in thienodiazepine and benzodiazepine derivatives.
The structural and electronic characteristics as well as the anticonvulsant properties and benzodiazepine receptor binding of thieno[3,4-b][1,4]diazepine and 1,5-benzodiazepine derivatives are compared and discussed. The data obtained suggest that the electronic rather than the structural properties appear mainly responsible for the variant degree of anticonvulsant activity exhibited by the tested compounds.
Chimirri
A
A
Dipartimento Farmaco-Chimico, Università di Messina, Italy.
Gitto
R
R
Grasso
S
S
Zappalà
M
M
De Sarro
A
A
Battista De Sarro
G
G
D000161:Acoustic Stimulation; D000818:Animals; D014151:Anti-Anxiety Agents; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001381:Azepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001570:Benzodiazepinones / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D000078306:Clobazam; D005445:Flunitrazepam / Q000493:pharmacokinetics; D008055:Lipids / Q000737:chemistry; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008811:Mice, Inbred DBA; D010433:Pentylenetetrazole; D051381:Rats; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013329:Structure-Activity Relationship
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001381:Azepines; D001570:Benzodiazepinones; D008055:Lipids; D001569:Benzodiazepines; D000078306:Clobazam; D005445:Flunitrazepam; D010433:Pentylenetetrazole