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XB-ART-1560
Bioorg Med Chem Lett 2005 Oct 01;1519:4286-90. doi: 10.1016/j.bmcl.2005.06.056.
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Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes.

Vrudhula VM , Dasgupta B , Boissard CG , Gribkoff VK , Santone KS , Dalterio RA , Lodge NJ , Starrett JE .


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Quinolinone 1 is a potent maxi-K potassium channel opener. In an effort to design analogs of 1 with a better inhibitory profile toward the CYP2C9 isozyme, the two acidic sites were chemically modified independently to generate a number of analogs. These analogs were evaluated as maxi-K channel openers in vitro using Xenopus laevis oocytes expressing cloned hSlo maxi-K channels. Compounds 15, 17, and 19 showed potent activity as maxi-K channel openers and were further evaluated for inhibition of the activity of the CYP2C9 isozyme. Compounds 17 and 19 showed diminished inhibitory potency against 2C9 and also against a panel of other more common CYP isozymes.

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Species referenced: Xenopus laevis
Genes referenced: cyp2c9 cyp4b1