Journal of medicinal chemistry · 2007
Pyridazinoquinolinetriones as NMDA glycine-site antagonists with oral antinociceptive activity in a model of neuropathic pain.
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Bare Thomas M, Brown Dean G, Horchler Carey L, Murphy Megan, Urbanek Rebecca A, Alford Vernon, Barlaam Christine, Dyroff Martin C, Empfield James B, Forst Janet M, Herzog Keith J, Keith Richard A, Kirschner Alan S, Lee Chi-Ming C, Lewis Joseph, McLaren Frances M, Neilson Kathy L, Steelman Gary B, Trivedi Shephali, Vacek Edward P, Xiao Wenhua
Аннотация
A series of 7-chloro-2,3-dihydro-2-[1-(pyridinyl)alkyl]-pyridazino[4,5-b]quinoline-1,4,10(5H)-triones were synthesized and found to have potent activity at the glycine site of the NMDA receptor. In some cases, these compounds possessed poor aqueous solubility that may have contributed to poor rat oral bioavailability. Subsequently, compounds have been identified with improved aqueous solubility and oral bioavailability. Several of these compounds were examined in a rat chronic constrictive injury (CCI) model of neuropathic pain and found to have potent activity when dosed orally.