These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Synthesis and anticonvulsant activity of 1,3-dihydro-5-phenyl-2H-pyrido[3,2-e]-1,4-diazepin-2-ones.
    Author: Fiakpui CY, Knaus EE.
    Journal: Drug Des Discov; 1993; 10(3):173-81. PubMed ID: 8268390.
    Abstract:
    1,3-Dihydro-5-phenyl-2H-pyrido[3,2-e]-1,4-diazepin-2-ones (11-13), in which the chlorophenyl ring of 7-chloro-1,4-benzodiazepin-2-ones is replaced by a pyridyl ring, were synthesized and evaluated as anticonvulsants using subcutaneous pentylenetetrazole (scPTZ) and maximal electroshock (MES) induced seizure screening tests. A methyl substituent at the N-1 and/or C-3 position of the diazepin-2-one ring system was not a determinant of scPTZ activity, but the 1,3-dimethyl derivative (13) was more potent than the parent 1,3-unsubstituted compound (11) in the MES screen. 1,3-Dihydro-1,3-dimethyl-5-phenyl-2H-pyrido[3,2-e]-1,4-diazepin-2- one (13) inhibited sc bicuculline and sc picrotoxin induced seizures, but it did not inhibit in vitro benzodiazepine binding which suggests it may act by a different mechanism of action. In the mouse Phase II scPTZ screen all compounds tested were less active than clonazepam but more active than valproic acid.
    [Abstract] [Full Text] [Related] [New Search]