[摘要]：A novel and robust scaffold for highly active PPAR alpha agonists based on the 2-mercaptohexanoic acid substructure is presented. Systematic structural variation of the substitution pattern of the phenolic backbone yielded detailed SAR especially of ortho and meta substituents. We corroborated the importance of the sulfur atom as well as of the n-butyl chain for PPAR alpha activity in the 2-mercaptohexanoic acid head group by preparation of carbon analogs and alpha-unsubstituted derivatives. Compound 10 represents a low nano molar active PPAR alpha activator with excellent selectivity towards PPAR gamma. (C) 2009 Elsevier Ltd. All rights reserved.
