Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines.
Analogues of bromazepam [7-bromo-1,3-dihydro-5(2-pyridyl)-2H-1,4-benzodiazepin-2-one, A], which is a clinically useful minor tranquilizer, have been prepared by replacing the 2-pyridyl group at position 5 with 4-pyrimidyl (5), 2-pyrazinyl (8), 2,5-dimethylpyrazin-3-yl (10), and 2-pyrimidyl (12) groups. Low to moderate CNS activities in both mice and cat were found for all the new compounds. For the screening procedures used, the 2-pyrimidyl-substituted derivatives were found to be the most active new analogues although none of the activities exceeded those observed for bromazepam.
D000374:Aggression / Q000187:drug effects; D000818:Animals; D000927:Anticonvulsants; D001522:Behavior, Animal / Q000187:drug effects; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D002415:Cats; D004597:Electroshock; D006801:Humans; D051379:Mice; D009126:Muscle Relaxation / Q000187:drug effects; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D011719:Pyrazines / Q000138:chemical synthesis / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology
D000927:Anticonvulsants; D011719:Pyrazines; D011743:Pyrimidines; D001569:Benzodiazepines; D010433:Pentylenetetrazole