3-Amino-1,5-benzodiazepinones: Potent, state-dependent sodium channel blockers with anti-epileptic activity

Authors :: Hoyt, Scott B.
London, Clare
Wyvratt, Matthew J.
Fisher, Michael H.
Cashen, Doreen E.
Felix, John P.
Garcia, Maria L.
Li, Xiaohua
Lyons, Kathryn A.
Euan MacIntyre, D.
Martin, William J.
Priest, Birgit T.
Smith, McHardy M.
Warren, Vivien A.
Williams, Brande S.
Kaczorowski, Gregory J.
Parsons, William H.
Source :: Bioorganic & Medicinal Chemistry Letters. Mar2008, Vol. 18 Issue 6, p1963-1966. 4p.
Publication Year :: 2008
Abstract: Abstract: A series of 3-amino-1,5-benzodiazepinones were synthesized and evaluated as potential sodium channel blockers in a functional, membrane potential-based assay. One member of this series displayed subnanomolar, state-dependent sodium channel block, and was orally efficacious in a mouse model of epilepsy. [Copyright &y& Elsevier]

Subjects :: *ION channels
*SODIUM channels
*DEVELOPMENTAL disabilities
*BRAIN diseases

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