Synthesis and pharmacological properties of 1-[2-hydroxy-3-(4-o,m,p-halogenophenyl)- and 3-(4-m-chlorophenyl)-1-piperazinyl]propyl derivatives of amides of 7-methyl-3-phenyl-2,4-dioxo-1,2,3,4-tetrahydropyrido [2,3-d]pyrimidine-5-carboxylic acid with analgesic and sedative activities.
Synthesis of 1-[2-hydroxy-3-(4-o,m,p-halogenophenyl)- and 3-(4-m-chlorophenyl)-1-piperazinyl]propyl derivatives of amides of 7-methyl-3-phenyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-5-carboxylic acid (18, 20-23, 25, 27-30 and 19, 24, 26) is described. All substances were active as analgesic agents in "writhing syndrome" test and except of 18 and 23 they acted stronger than acetylsalicylic acid. All final derivatives tested significantly suppressed the spontaneous locomotor activity of mice.
Department of Chemistry of Drugs, Wrocław University of Medicine, Tamka 1, 50-137 Wrocław, Poland. fastola@poczta.onet.pl
Aleksandra
A
Sabiniarz
Helena
H
Sladowska
Barbara
B
Filipek
Jacek
J
Sapa
Magdalena
M
Dudek
Katarzyna
K
Slepokura
D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology; D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D001241:Aspirin / Q000494:pharmacology; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000494:pharmacology*; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis / Q000494:pharmacology; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010146:Pain / Q000188:drug therapy; D010147:Pain Measurement; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000577:Amides; D000700:Analgesics; D002264:Carboxylic Acids; D006993:Hypnotics and Sedatives; D011743:Pyrimidines; D001241:Aspirin