3-Trifluoromethyl-4-nitro-5-arylpyrazoles are novel K ATP channel agonists

…, C Townsend, MC McKay, D Garrido, CM Terry…

文献索引：Peat, Andrew J.; Townsend, Claire; McKay, M. Craig; Garrido, Dulce; Terry, Christopher M.; Wilson, Jayme L. R.; Thomson, Stephen A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 3 p. 813 - 816

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被引用次数: 11

摘要

This communication describes the discovery and synthesis of a series of 3-trifluoromethyl-4- nitro-5-arylpyrazoles as potent KATP channel agonists. The most potent compound reported is ca. 100-fold more potent than diazoxide and exhibits selectivity for the SUR1 KATP 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.