Fluorinated quinazolones III: synthesis and CNS depressant activity of fluorinated quinazolone derivatives.
The synthesis of 2-allylthio-3-(4'-fluorophenyl)-5,6,7,8-tetrafluoro-4-quinazolone, 2-n-propylthio-3-(4'-fluorophenyl)-5,6,7,8-tetrafluoro-4-quinazolone, 3-(4'-bromophenyl)-5,6,7,8-tetrafluoro-2,4-quinazolinedithione, and seven fluorinated 2-alkyl/phenyl-3-aryl-4(3H)-quinazolones is described. The synthesized compounds were screened for CNS depressant activity using pentobarbital sleeping time, pentylenetetrazol convulsions, and condition avoidance test as the parameters. Most of the screened compounds exhibited significant depressant activity.
D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects*; D003864:Depression, Chemical; D005260:Female; D005461:Fluorine; D008297:Male; D051379:Mice; D010424:Pentobarbital / Q000494:pharmacology; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D011799:Quinazolines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D012890:Sleep / Q000187:drug effects; D013997:Time Factors
D011799:Quinazolines; D005461:Fluorine; D010424:Pentobarbital; D010433:Pentylenetetrazole