XB-ART-4067
Bioorg Med Chem Lett
2004 Feb 09;143:813-6. doi: 10.1016/j.bmcl.2003.10.066.
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3-trifluoromethyl-4-nitro-5-arylpyrazoles are novel K(ATP) channel agonists.
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This communication describes the discovery and synthesis of a series of 3-trifluoromethyl-4-nitro-5-arylpyrazoles as potent K(ATP) channel agonists. The most potent compound reported is ca. 100-fold more potent than diazoxide and exhibits selectivity for the SUR1 K(ATP) channel subtype. The 4-nitro substitutent on the pyrazole ring was required for activity, and limited SAR suggests that the de-protonated pyrazole maybe the active species.
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Species referenced: Xenopus laevis
Genes referenced: abcc8