Synthesis and analgesic activity of some quinazoline analogs of anpirtoline.
New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, quinazoline, 7-chloroquinoline, and 7-chloroquinazoline 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 4e-4g, and 4l are at least comparable to that of clinically used drugs flupirtine and tramadol under the same conditions.
Rádl
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Research Institute of Pharmacy and Biochemistry, Kourimska 17, 13060 Prague, Czech Republic.
Hezky
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P
Proska
J
J
Krejcí
I
I
D000631:Aminopyridines / Q000494:pharmacology; D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D006358:Hot Temperature; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D010146:Pain / Q000503:physiopathology*; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011930:Reaction Time; D044302:Receptor, Serotonin, 5-HT1B; D011985:Receptors, Serotonin / Q000502:physiology; D044263:Receptors, Serotonin, 5-HT1; D013329:Structure-Activity Relationship; D014147:Tramadol / Q000494:pharmacology
D000631:Aminopyridines; D000700:Analgesics; D010880:Piperidines; D011725:Pyridines; D011799:Quinazolines; D044302:Receptor, Serotonin, 5-HT1B; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; C075631:anpirtoline; D014147:Tramadol; C034161:flupirtine