Zettl, Heiko and Steri, Ramona and Lämmerhofer, Michael and Schubert-Zsilavecz, Manfred (2009) Discovery of a novel class of 2-mercaptohexanoic acid derivatives as highly active PPAR[alpha] agonists. Bioorganic & Medicinal Chemistry Letters, 19 (15). pp. 4421-4426.
Full text is not hosted in this archive but may be available via the Official URL, or by requesting a copy from the corresponding author.
Official URL: http://www.sciencedirect.com/science/article/B6TF9...
A novel and robust scaffold for highly active PPARα 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 PPARα activity in the 2-mercaptohexanoic acid head group by preparation of carbon analogs and α-unsubstituted derivatives. Compound 10 represents a low nano molar active PPARα activator with excellent selectivity towards PPARγ.
|Uncontrolled Keywords:||PPAR; 2-Mercaptohexanoic acid; SAR; PPARα agonists|
|Subjects:||Biomedical Science > Nanomedicine|
|Deposited On:||04 Aug 2009 10:47|
|Last Modified:||04 Aug 2009 10:47|
Repository Staff Only: item control page