Acylated derivatives of 1,5-benzodiazepines. Part II.
Acylated derivatives of 4-methyl-1H-tetrahydro-1,5-benzodiazepin-2-one (1) and of 2-methyl-4-phenyl-1H-tetrahydro-1,5-benzodiazepino-2-carboxylic acid ethyl ester (10) were synthesized and preliminarily tested on their central activity. Acylation was carried out with alpha, beta-unsaturated acid chlorides, dicarboxylic acid monoester monochlorides, and dicarboxylic acid dichlorides. Compounds 2, 3, 11 and 12 had analgesic, compounds 4, 11 and 12--anticonvulsant, and compounds 3 and 11--antiaggressive properties.
Nawrocka
W
W
Department of Technology of Drugs, Medical Academy, Wrocłøaw, Poland.
Liszkiewicz
H
H
Nawojski
A
A
Wilimowski
M
M
Kedzierska-Goździk
L
L
Barczyńska
J
J
Wojewódzki
W
W
Duś
E
E
Szelag
A
A
Rutkowska
M
M
D000215:Acylation; D000818:Animals; D001569:Benzodiazepines / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D005260:Female; D006358:Hot Temperature; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy*
D001569:Benzodiazepines; D010433:Pentylenetetrazole