1.
J Med Chem
; 20(10): 1312-7, 1977 Oct.
Article
in English
| MEDLINE
| ID: mdl-561846
ABSTRACT
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.
Subject(s)
Benzodiazepines/chemical synthesis , Aggression/drug effects , Animals , Anticonvulsants , Behavior, Animal/drug effects , Benzodiazepines/pharmacology , Cats , Electroshock , Humans , Mice , Muscle Relaxation/drug effects , Pentylenetetrazole/antagonists & inhibitors , Pyrazines/chemical synthesis , Pyrazines/pharmacology , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology
2.
J Med Chem
; 18(2): 222-4, 1975 Feb.
Article
in English
| MEDLINE
| ID: mdl-1120995