863225-76-7Relevant academic research and scientific papers
Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes
Vrudhula, Vivekananda M.,Dasgupta, Bireshwar,Boissard, Christopher G.,Gribkoff, Valentin K.,Santone, Kenneth S.,Dalterio, Richard A.,Lodge, Nicholas J.,Starrett Jr., John E.
, p. 4286 - 4290 (2007/10/03)
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.
