Synthesis and analgesic activity of some condensed analogs of anpirtoline.
New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, isoquinoline, quinazoline, and phthalazine nuclei, have been synthesized. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. The analgesic activity of compounds 7d, 8b, 8c, and 8e are at least comparable to that of the clinically used drugs flupirtine and tramadol under the same conditions.
Research Institute of Pharmacy and Biochemistry, Prague, Czech Republic.
S
S
Rádl
L
L
Kovárová
P
P
Hezky
V
V
Vosátka
O
O
Königová
J
J
Proska
I
I
Krejcí
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D008297:Male; D051379:Mice; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000700:Analgesics; D010880:Piperidines; D011725:Pyridines; C075631:anpirtoline