| Literature DB >> 14741296 |
Andrew J Peat1, Claire Townsend, M Craig McKay, Dulce Garrido, Christopher M Terry, Jayme L R Wilson, Stephen A Thomson.
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.Entities:
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Year: 2004 PMID： 14741296 DOI： 10.1016/j.bmcl.2003.10.066
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823