Synthesis of some N-substituted 3,4-pyrroledicarboximides as potential CNS depressive agents.
As a continuation of our work on N-[4-aryl(heteroaryl)piperazin-1-ylalkyl]-3,4-pyrro ledicarboximides, which were characterized by strong analgesic activity and CNS depressive action, several novel N-substituted 3,4-pyrroledicarboximides were prepared and eleven representatives were examined in a series of in vivo CNS tests. A few of these compounds displayed a similar profile of biological selectivity to that of 3,4-pyrroledicarboximides described previously; their structure-activity relationships are discussed.
Malinka
W
W
Department of Chemistry of Drugs, Wrocław Medical University, Poland.
Sieklucka-Dziuba
M
M
Rajtar
G
G
Rejdak
R
R
Rejdak
K
K
Kleinrok
Z
Z
D000661:Amphetamine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D002492:Central Nervous System Depressants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000697:Central Nervous System Stimulants / Q000037:antagonists & inhibitors / Q000494:pharmacology; D005260:Female; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010146:Pain / Q000188:drug therapy / Q000523:psychology; D011597:Psychomotor Performance / Q000187:drug effects; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D013055:Spectrophotometry, Infrared
D018712:Analgesics, Non-Narcotic; D000927:Anticonvulsants; D002492:Central Nervous System Depressants; D000697:Central Nervous System Stimulants; D011758:Pyrroles; D000661:Amphetamine