Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-γ/δ dual agonists

HJ Gim, YJ Cheon, JH Ryu, R Jeon

文献索引：Gim, Hyo Jin; Cheon, Ye-Jin; Ryu, Jae-Ha; Jeon, Raok Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 10 p. 3057 - 3061

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被引用次数: 12

摘要

Abstract A series of benzoxazole or benzothiazole containing indole analogs, 6- alkoxyindole-2-carboxylic acids and 5-alkoxy-3-indolylacetic acids, were synthesized as novel candidates of PPARγ/δ dual agonists and their ligand activities for PPAR subtypes (α, γ, and δ) were investigated. In transient transactivation assay, several compounds activated PPARγ and δ with little activity of PPARα. Putative binding mode of the compounds 1a and ...