2. Academic Validation
  3. 3-trifluoromethyl-4-nitro-5-arylpyrazoles are novel K(ATP) channel agonists

3-trifluoromethyl-4-nitro-5-arylpyrazoles are novel K(ATP) channel agonists

  • Bioorg Med Chem Lett. 2004 Feb 9;14(3):813-6. doi: 10.1016/j.bmcl.2003.10.066.
Andrew J Peat 1,  Claire Townsend,  M Craig McKay,  Dulce Garrido,  Christopher M Terry,  Jayme L R Wilson,  Stephen A Thomson
Affiliations

Affiliation

  • 1 GlaxoSmithKline Research & Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA.
PMID: 14741296 DOI: 10.1016/j.bmcl.2003.10.066
Abstract

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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