Investigations on the synthesis and pharmacological properties of N-substituted derivatives of 4-alkoxy-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones.
Synthesis of N-substituted derivatives of 4-alkoxy-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones (10-14, 18-21) is described. In the "writhing syndrome" test all compounds studied exhibited potent analgesic activity which was superior than that of acetylsalicylic acid. In the "hot plate" test imides 10, 12, 13, 18-20 acted also stronger than aspirin. Furthermore all compounds tested significantly suppressed the spontaneous locomotor activity of mice and prolonged barbiturate sleep of these animals.
Sladowska
Helena
H
Department of Chemistry of Drugs, Wrocław University of Medicine, Tamka 1, 50-137 Wrocław, Poland. helena@bf.uni.wroc
Filipek
Barbara
B
Szkatuła
Dominika
D
Sapa
Jacek
J
Bednarski
Marek
M
Ciołkowska
Marta
M
D000698:Analgesia; D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000700:Analgesics; D011758:Pyrroles