title: Synthesis and pharmacological evaluation of N-(dimethylamino)ethyl derivatives of benzo- and pyridopyridazinones.
abstract: 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.
authors.affiliation: Department of Pharmacodynamics, Medical University of Lodz, Lodz, Poland. wpakulska@pharm.am.lodz.pl
authors.forename: Wanda
authors.initials: W
authors.lastname: Pakulska
authors.forename: Zbigniew
authors.initials: Z
authors.lastname: Malinowski
authors.forename: Aleksandra K
authors.initials: AK
authors.lastname: Szczesniak
authors.forename: Elzbieta
authors.initials: E
authors.lastname: Czarnecka
authors.forename: Jan
authors.initials: J
authors.lastname: Epsztajn
mesh_terms: 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
chemical_list: D018712:Analgesics, Non-Narcotic; D010793:Phthalazines; D011724:Pyridazines; D004177:Dipyrone