Synthesis and pharmacological evaluation of N-(dimethylamino)ethyl derivatives of benzo- and pyridopyridazinones.
New N-(dimethylamino)ethyl derivatives of phthalazinones and pyridopyridazinones 7, 9 were synthesized and assayed as potential analgesic agents in the hot-plate, tail-flick, and writhing tests. Pharmacological assay demonstrated that eight (in ten) of the newly synthesized compounds showed antinociceptive activity. Especially, 2-[2-(dimethylamino)ethyl]-4-phenyl-2H-phthalazin-1-one 7a showed remarkably higher antinociceptive activity in all tests. This is connected with influence on supraspinal, spinal, and peripheral structures. The decreased sensitivity to the pain stimulus in the hot-plate was higher than that of metamizole.
Pakulska
Wanda
W
Department of Pharmacodynamics, Medical University of Lodz, Lodz, Poland. wpakulska@pharm.am.lodz.pl
Malinowski
Zbigniew
Z
Szczesniak
Aleksandra K
AK
Czarnecka
Elzbieta
E
Epsztajn
Jan
J
D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D004177:Dipyrone; D004353:Drug Evaluation, Preclinical; D051379:Mice; D017288:Pain Threshold / Q000187:drug effects; D010793:Phthalazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D018712:Analgesics, Non-Narcotic; D010793:Phthalazines; D011724:Pyridazines; D004177:Dipyrone